Publications Resulting from Collaborations

1. Publications from Parke, Davis Laboratories (1961-1971)
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  • S. Hanessian, W. Regan, D. Watson, T.H. Haskell, "Isolation and characterization of the antigenic components of a new heptavalent Pseudomonas vaccine", Nature New Bio.(Lond.) 1971, 229:209-210.
  • S. Hanessian et A.P.A. Staub, "The Diaxial Diequatorial Rearrangement in the Carbohydrate Series", Carbohydrate Res. 1970, 14, 424.
  • S. Hanessian et G. Schütze, "Synthetic Penicillins Derived from Benznorcaradienecarboxylic Acids", J. Med. Chem. 1969, 12, 529.
  • S. Hanessian et G. Schütze, "Synthetic Penicillins Derived from Cycloheptatrienecarboxylic Acids", J. Med. Chem. 1969, 12, 527.
  • S. Hanessian et G. Schütze, "Synthesis of DL-2(2,4,6-Cycloheptatrien-l-yl) glycine", J. Med. Chem. 1969, 12, 347.
  • S. Hanessian et G. Schütze, "A Study of Some Substituted Cycloheptatriene Carboxylic Acid by Nuclear Magnetic Resonance Spectroscopy", J. Org. Chem. 1969, 34, 3196.
  • S. Hanessian et N. R. Plessas, "Reactions of Carbohydrates with (Halomethylene)dimethyliminium Halides and Related Reagents.  Synthesis of Some Chlorodeoxy Sugars", J. Org. Chem. 1969, 34, 2163.
  • S. Hanessian et N. R. Plessas, "The Reaction of O-Benzylidene Sugars with N-Bromosuccinimide.  IV. Neighboring Group Effects and Rearrangements", J. Org. Chem. 1969, 34, 1053.
  • S. Hanessian et N.R. Plessas, "The Reaction of O-Benzylidene Sugars with N-Bromosuccinimide.  III.  Applications to the Synthesis of Aminodeoxy and Deoxy Sugars of Biological Importance", J. Org. Chem. 1969, 34, 1045.
  • S. Hanessian et N.R. Plessas, "The Reaction of O-Benzylidene Sugars with N-Bromosuccinimide.  II. Scope and Synthetic Utility in the Methyl 4,6-O-Benzylidene-hexopyranosides Series", J. Org. Chem. 1969, 34, 1035.
  • S. Hanessian, "Sugar Lactams. III. Synthesis of Five, Six et Seven Membered Analogs", J. Org. Chem. 1969, 34, 675.
  • D.C. De Jongh, T. Radford, J.D. Hribar, S. Hanessian, M. Bieber, G. Dawson et C.C. Sweeley, "Analysis of Trimethylsilyl Derivatives of Carbohydrates by Gas Chromatography and Mass Spectrometry", J. Am. Chem. Soc. 1969, 91, 1728.
  • S. Hanessian et N.R. Plessas, "Synthesis of Unsaturated Sugars Containing Vinylic Substituents", Chem. Commun. 1968, 706.
  • S. Hanessian, "Some Approaches to the Synthesis of Halodeoxy Sugars", Advances in Chemistry Series, 1968, 74, 159.
  • D.C. De Jongh, J.D. Hribar et S. Hanessian, "Mass Spectrometry in Carbohydrate Chemistry.  Glycosides and O-Isopropylidene Ketals of Deoxy Sugars", Advances in Chemistry Series, 1968, 74, 202..
  • S. Hanessian, "Selective Hydrolysis of Amide Bonds in Acetamido Deoxy Sugars: O-Ethyl Acetamidium Fluoroborates", Tetrahedron Lett. 1967, 16, 1549.
  • S. Hanessian, "Neighboring Group Participation Across a Furanose Ring.  Synthesis of 5-Acetamido-5-Deoxy-D-Lyxopyranose from D-Arabinose Precursors", J. Org. Chem. 1967, 32, 163.
  • D.C. De Jongh, J.D. Hribar, S. Hanessian et P.W.K. Woo, "Mass Spectrometric Studies on Amino Cyclitol Antibiotics", J. Am. Chem. Soc. 1967, 89, 3364.
  • S. Hanessian et N.R. Plessas, "A New Synthesis of Chlorodeoxy Sugars", Chem. Commun. 1967, 1152.
  • S. Hanessian et J.S. Kaltenbronn, "Synthesis of a Bromine-Rich Marine antibiotic", J. Am. Chem. Soc. 1966, 88, 4509.
  • D.C. De Jongh et S. Hanessian, "Characterization of Deoxy Sugars by Mass Spectrometry", J. Am. Chem. Soc. 1966, 88, 3114.
  • S. Hanessian, "Ring Contraction and Epimerization during a Displacement Reaction of a Hexose Sulphonate", Chem. Commun. 1966, 796.
  • S. Hanessian, "Synthesis of Hydroxypiperidines from Carbohydrate Precursors", Chem. Ind. 1966, 2126.
  • S. Hanessian, "The Reaction of O-Benzylidene Sugars with N-Bromosuccinimide.  I. Methyl 4,6-O-Benzylidenehexopyranosides", Carb. Res. 1966, 2, 86.
  • S. Hanessian, D.C. De Jongh et J.A. McCloskey, "Further Evidence on the Structure of Cordycepin", Biochim. Biophys. Acta, 1966, 117, 480.
  • S. Hanessian, "Deoxy Sugars", Advances in Carbohydrate Chemistry 1966, 21, 143.
  • S. Hanessian et T.H. Haskell, "Synthesis and Characterization of 3,6-Diamino-3,6- Dideoxy-D-Idose", J. Org. Chem. 1965, 30, 1080.
  • D.C. De Jongh et S. Hanessian, "Characterization of Amino Sugars by Mass Spectrometry", J. Am. Chem. Soc.. 1965, 87, 3744.
  • D.C. De Jongh et S. Hanessian, "Assignment of the Position of Amino Groups in Amino Sugars by Mass Spectrometry", J. Am. Chem. Soc. 1965, 87, 1408.
  • S. Hanessian, "Reductive Rearrangement of 5-Azido-5-Deoxy-pentoses. A New Synthesis of Sugars Containing Nitrogen in the Ring", Chem. Ind. 1965, 1296.
  • S. Hanessian, "Sugars Containing Nitrogen in The Ring.  4,5-Diacetamido- 4,5-Dideoxy-L-Xylopyranose and the Anomeric 4-Acetamido-4,5-Dideoxy-D-Xylofuranoses", Carb. Res. 1965, 1, 178.
  • S. Hanessian et T. H. Haskell, "Configuration of the Anomeric Linkages in Amicetin", Tetrahedron Lett. 1964, 36, 2451.
  • S. Hanessian et T.H. Haskell, "Sugar Lactams.  II. 4-Amino-4-Deoxy-D-Erythronolactam and Related Products", J. Heterocyclic Chem. 1964, l, 57.
  • S. Hanessian et T. H. Haskell, "Sugar Lactams. I. 5-Amino-5-Deoxy-D-Ribonolactam and Related Products", J. Heterocyclic Chem. 1964, l, 55.
  • S. Hanessian et T.H. Haskell, "Structural Studies on Staphylococcal Polysaccharide Antigen", J. Biol. Chem. 1964, 239, 2758.
  • T.H. Haskell et S. Hanessian, "The Purification and Characterization of a New Active Immunizing Polysaccharide Prepared from Staphylococcus aureus", Biochim. Biophys. Acta, 1964, 83, 35..
  • T.H. Haskell et S. Hanessian, "A New Staphylococcal Antigen" Nature 1963, 199, 1074.

2. Publications Resulting from Collaborations by Therapeutic Area(1973-present)

Inhibitors of BACE 1 (Alzheimer’s disease: Novartis Pharma, Basel)
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  • S. Hanessian, M. Brassard, “Stereoselective Synthesis of Constrained Oxacyclic Hydroxyethylene Isosteres of Aspartyl Protease Inhibitors II. Nitroaldol Methodology toward 2,3-Substituted Tetrahydrofurans”, Tetrahedon 2004, 60, 7261.
  • S. Hanessian, H Yun, Y. Hou, G. G. Yang, M. Bayrakdarian, E. Therrien, N. Moitessier, S. Roggo, S. Veenstra, M. Tintlenot-Blomley, J-M. Rondeau, C. Ostermeier, A. Strauss, P. Ramage P. Paganetti, U. Neumann, C. Betschart, “Structure-based Design, Synthesis, and Memapsin 2 (BACE) Inhibitory Activity of Carbocyclic Heterocyclic Peptidomimetics” J. Med. Chem. 2005, 48, 5175.
  • S. Hanessian, Y. Hou, “Stereoselective Synthesis of Constrained Hydroxyethylene. Isosteres of Aspartyl Protease Inhibitors I. Aldol and Mukaiyama Aldol Methodologies”, J. Org. Chem. 2005. 70, 6735.
  • S. Hanessian, H. Yun, Y. Hou, M. Tintelnot-Blomley, “Stereoselective Synthesis of Constrained Azacyclic Hydroxyethylene Isosteres as Aspartic Protease Inhibitors: Dipolar Cycloaddition and Related Methodologies toward Branched Pyrrolidine and Pyrrolidinone Carboxylic Acids”, J. Org. Chem. 2005, 70, 6746.
  • S. Hanessian, H Yun, Y. Hou, G. G. Yang, M. Bayrakdarian, E. Therrien, N. Moitessier, S. Roggo, S. Veenstra, M. Tintlenot-Blomley, J-M. Rondeau, C. Ostermeier, A. Strauss, P. Ramage P. Paganetti, U. Neumann, C. Betschart, “Structure-based Design, Synthesis, and Memapsin 2 (BACE) Inhibitory Activity of Carbocyclic Heterocyclic Peptidomimetics” J. Med. Chem. 2005, 48, 5175.
  • N. Moitessier, E. Therrien, S. Hanessian, “A Method for Induced-fit Docking, Scoring and Ranking of Flexible ligands. Application to Peptidic and Pseudopeptidic BACE-1 Inhibitors.” J. Med. Chem. 2006, 49, 588.
  • S. Hanessian, G. Yang, J.-M. Rondeau, U. Neumann, C. Betschart, and M. Tintelnot-Blomley, “Structure-Based Design and Synthesis of Macroheterocyclic Peptidomimetic Inhibitors of the Aspartic Protease β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE)”, J. Med. Chem. 2006, 49, 4544.
  • S. Hanessian, G. Charron, A. Billich, D. Guerini, “Constrained azacyclic cyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors”, Bioorg. Med. Chem. Lett. 2007, 17, 491.
  • S. Hanessian, Z. Shao, C. Betschart, J-M. Rondeau, U. Neumann, M. Tintelnot-Blomley, " Structure-based Design and Synthesis of Novel P2/P3 Modified, Non-Peptidic β-Secretase (BACE-1) Inhibitors", Bioorg. Med. Chem. Lett. 2010, 20, 1924.
  • S. Hanessian, D. K. Maji, S. Govindan, R. Matera, M. Tintelnot-Blomley, "Substrate-controlled, and organocatalytic asymmetric syntheses of carbocyclic amino acid dipeptide mimetics", J. Org. Chem. 2010, 75, 2861.
Aminoglycoside antibiotics (Antibacterial: Ibis Therapeutics, Carlsbad, Ca, Achaogen Inc., South San Francisco, CA )
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  • S. Hanessian, M. Tremblay, A. Kornienko and N. Moitessier, “Design, Modeling and Synthesis of a Functionalized Paromamine Library”, Tetrahedron 2001, 57, 3255.
  • S. Hanessian, A. Kornienko, and E. E. Swayze, “Probing the functional requirements of the L-haba side-chain of amikacin: synthesis, 16S A-site rRNA binding, and antibacterial activity”, Tetrahedron 2003, 59, 995.
  • S. Hanessian, M. Tremblay, and E. E. Swayze, “Tobramycin analogues with C-5 aminoalkyl ether chains intended to mimic rings III and IV of paromomycin”, Tetrahedron 2003, 59, 983.
  • S. Hanessian, J. Szychowski, S. Adhikari, E. Westhof, B. François, E. Swayze and R. H. Griffey, “Antibacterial Aminoglycosides with a Modified Mode of Bonding to the Ribosomal RNA Decoding Site”, Angew. Chem. Int. Ed. 2004, 43, 6735.
  • N. Moitessier, E. Westhof, S. Hanessian, “Docking of Aminoglycosides to Hydrated and Flexible RNA” J. Med. Chem. J. Med. Chem. 2006, 49, 1023.
  • J. Kondo, K. Pachamuthu, B. François, J. Szychowski, S. Hanessian, E. "Westhof, Crystal Structure of the Bacterial Ribosomal Decoding Site Complexed with a Synthetic Doubly Functionalized Paromomycin Derivative: a New Specific Binding Mode to an A-Minor Motif enhances in vitro Antibacterial Activity." ChemMedChem 2007, 2, 1631.
  • S. Hanessian, S. Adhikari, J. Szychowski, P. Kandasamy, X. Wang, M. T. Migawa, R. H. Griffey, E. E. Swayze, “Probing the Ribosomal RNA A-site with Functionally Diverse Analogues of Paromomycin – Synthesis of Ring I Mimetics”, Tetrahedron 2007, 63, 874.
  • S. Hanessian, J. Szychowski, S. S. Adhikari, G. Vasquez, P. Kandasamy, E. E. Swayze, M. T. Migawa, B. François, J. Wirmer-Bartoschek, E. Westhof, “Structure-based Design, Synthesis and A-site rRNA Co-crystal Complexes of Functionally Novel Aminoglycoside Antibiotics I: C-2” Ether Analogues of Paromomycin”, J. Med. Chem. 2007, 50, 2352.
  • S. Hanessian, J. Szychowski, P. Kandasamy, N. B. Campos-Reales Pineda, A. Furtos, J. W. Keillor, “6-Hydroxy to 6'''-Amino Tethered Ring-to-Ring Macrocyclic Aminoglycosides as Probe for APH(3’)IIIa Kinase”, Bioorg. Med. Chem. Lett. 2007, 17, 3221.
  • S. Hanessian, J. Szychowski, J.P. Maianti, "Synthesis and Comparative Antibacterial Activity of Verdamicin C2 and C2A. A New Oxidation of Primary Allylic Azides in Dihydro[2H]pyrans", Org. Lett. 2009, 11, 429-432.
  • S. Hanessian, P. Kandasamy, J. Szychowski, A. Giguère, E. E. Swayze, M. T. Migawa, B. François, J. Wirmer-Bartoschek, J. Kondo and E. Westhof, "Structure-Based Design, Synthesis and A-site rRNA Co-Crystal Complexes ofAmphiphilic Novel Aminoglycoside Antibiotics with New Binding Modes: A Synergistic Hydrophobic Effect", Bioorg. Med. Chem. 2010, 20, 7097.
  • S. Hanessian; A. Giguère; J. Grzyb; J. P. Maianti, "Overcoming Staphylococcus aureus Aminoglycoside Resistance Mechanisms with a Functionally Desgined Neomycin Analog", ACS. MedChem. Lett. 2011, 2, 924.
  • S. Hanessian; J. P. Maianti, "Designed Hybrid Aminoglycoside Antibiotics – Applications of the Tsuji Palladium-Catalyzed Allylic Deoxygenation", Org. Lett. 2011, 13, 6476.
  • S. Hanessian; J. P. Maianti; V.L. Ly, B. Deschênes-Simard, "Structural and Kinetic Study of Self-Assembling Macrocyclic Dimer Natural Product Aminoglycoside 66-40C and Unatural Variants", Chemical Sciences 2012, 3, 249.
  • S. Hanessian; O. M. Saavedra; M. A. Vilchis-Reyes; A. M. Llaguno-Rueda "Synthesis of 4’-deoxy-4’-fluoro neamine and 4’-deoxy-4’-fluoro 4’epi-neamine" RSC MedChemComm. 2014, 5, 1166.
  • J. P. Maianti; H. Kanazawa, P. Dozzo, R. d. Matias. L. Feeney, E. S. Armstrong; D. J. Hildebrandt. T. R. Kane; M. J. Gliedt; A. A. Goldblum; M. S. Linsell. J. B. Aggen; J. Kondo; S. Hanessian "Toxicity Modulation, Resistance Enzyme Evasion, and A-Site X-ray Structure of Broad‑Spectrum Antibacterial Neomycin Analogs" – ACS Chem. Bio. 2014, 9, 2067.
  • J.P. Maianti; S. Hanessian "Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes" RSC MedChem Comm. 2016, 7, 170-176.
Agrochemical natural Products (Fungicides, herbicides, anthelmintics, anti-cancer: Syngenta, Basel, UK; ex. Ciba-Agro, Basel).
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  • S. Hanessian, J.-Y. Sancéau and P. Chemla, "Synthesis of Surrogate Structures Related to the Herbicidal Agent Hydantocidin", Tetrahedron 1995, 51, 6669.
  • S. Hanessian and R.Y. Yang, "Solution and Solid Phase Synthesis of 5-Alkoxyhydantoins with Three Fold Functional Diversity, Tetrahedron Lett. 1996, 37, 5835.
  • S. Hanessian, R.Y. Yang and J.Y. Sancéau, "Synthesis and Biological Evaluation of 1-N-Hydroxydantoin 5-Phosphates as Potential Fungicides", Can. J. Chem. 1997, 75, 712.
  • S. Hanessian, P.-P. Lu, J.-Y. Sancéau, P. Chemla, L. Prade, K. Gohda, R. Fonne-Pfister, “Design, Synthesis and X-ray Crystal Structure of an Enzyme Bound Bisubstrate Hybrid Inhibitor of Adenylosuccinate Synthetase”, Angew. Chemie Int. Ed. Engl. 1999, 38, 3159.
  • S. Hanessian and R. Machaalani “A Highly Stereocontrolled and Efficient Synthesis of α-and b-Pseudouridines” Tetrahedron Lett. 2003, 44, 8321.
  • S. Hanessian, S. Marcotte, R. Machaalani, G. Huang “Total Synthesis and Structural Confirmation of Malayamycin A. A Novel Bicyclic C-Nucleoside from Streptomyces”, Org. Lett. 2003, 5, 4277.
  • S. Hanessian, G. Huang, C. Chenel, R. Machaalani, O. Loiseleur, “Total Synthesis of N-Malayamycin A and Related Bicyclic Purine and Pyrimidine Nucleosides”, J. Org. Chem. 2005, 70, 6721.
  • O. Loiseleur, S. Hermann, G. Huang, R. Machaalani, P. Sellès, P. Crowley, and S. Hanessian, “A Scalable Synthesis of 1-Cytosinyl-N-malayamycin A: A Potent Fungicide, Org. Proc. Res. Dev. 2006, 10, 518.
  • S. Hanessian, S. Marcotte, R. Machaalani, G. Huang, J. Perron, O. Loiseleur, “Total Synthesis of Malayamycin A and Analogues”, Tetrahedron 2006, 62, 5201.
  • S. Hanessian, D. J. Ritson “Structure-based Organic Synthesis of a Tricyclic N-Malayamycin Analogue”, J. Org. Chem. 2006, 71, 9807.
  • O. Loiseleur, D. Ritson, M. Nina, P. Crowley, T. Wagner, and S. Hanessian, “Ring-Modified Analogues and Molecular Dynamics Studies to Probe the Requirements for Fungicidal Activities of Malayamycin A and its N-Nucleoside Variants”, J. Org. Chem. 2007, 72, 6353.
  • S. Hanessian, T. Focken, R. Oza, "Total Synthesis of Jerangolid A", Org Lett. 2010, 12, 3172.
  • S. Hanessian, T. Focken, X. Mi, D. Ritson, R. Oza and B. Chen, "Total Synthesis of Ambruticin S – Probing the Pharmacophoric Subunit", J. Org. Chem. 2010, 75, 5601.
Metalloprotease inhibitors; receptor agonists and antagonists ( Servier, France)

  • S. Hanessian, A. Griffin and P. V. Devasthale “Synthesis of Conformationally Constrained Potential Inhibitors of Mammalian Metalloproteinasees, Bioorg. Med. Chem. Lett. 1997, 7, 3119.
  • S. Hanessian, S. Bouzbouz, A. Boudon, G. C. Tucker, D. Peyroulan, “Picking the S1, S1’ and S2’ Pockets of Matrix Metalloproteinases. A Niche for Potent Acyclic Sulfonamide Inhibitors”, Bioorg. Med. Chem. Lett. 1999, 9, 1691.
  • S. Hanessian and L.-D. Cantin, “The Synthesis of Enantiomerically Pure Disubstituted Aziridines and N-AlkoxyAziridines”,Tetrahedron Lett. 2000, 41, 787.
  • S. Hanessian, N. Moitessier, and S. Wilmouth, “Tetrahydrofuran as a Scaffold for Peptidomimetics. Application to the Design and Synthesis of Conformationally Constrained Metalloproteinase Inhibitors”, Tetrahedron 2000, 56, 7643.
  • S. Hanessian, N. Moitessier, and E. Therrien, “Design and synthesis of MMP inhibitors guided by molecular modeling. Overview of the available structural data, comparative docking study and design of potentially selective inhibitors”, J. Computer-aided Molecular Design 2001, 15, 873.
  • S. Hanessian, N. Moitessier, C. Gauchet and M. Viau, “N-Aryl Sulfonyl Homocysteine Hydroxamate Inhibitors of Matrix Metalloproteinases: Further Probing of the S1, S1’ and S2’ Pockets”, J. Med. Chem. 2001, 44, 3066.
  • S. Hanessian, D. B. Mackay, and N. Moitessier, “Design and Synthesis of MMP inhibitors Guided by Molecular Modeling. Picking the MMP S1 Pocket Using Conformationally Constrained Inhibitors”, J. Med. Chem. 2001, 44, 3074.
  • S. Hanessian, N. Moitessier, and L.-D. Cantin, “Design and Synthesis of MMP Inhibitors Guided by Molecular Modeling. N-Arylsulfonylaziridine Hydroxamic Acids as Constrained Scaffolds”, Tetrahedron 2001, 57, 6885.
  • J. Jourquin, E. Tremblay, N. Décanis, G. Charton, S. Hanessian, A.-M. Chollet, T. Le Diguardher, M. Khrestchatisky and S. Rivera, "Neuronal activity-dependent increase of net MMP activity is associated with MMP-9-neurotoxicity after kainate", European Journal of Neuroscience 2003, 18, 1.
  • S. Hanessian and N. Moitessier, “Sulfonamide-Based Acyclic and Conformationally Constrained MMP Inhibitors: From Computed-Assisted Design to Nanomolar Compounds”, Curr. Topics in Med. Chem. 2004, 4, 1269.
  • C. Ogier, A. Bernard, A.-M. Chollet, T. Le Diguardher, S. Hanessian, G. Charton, M. Khrestchatisky, S. Rivera, “Matrix Metalloproteinase-2 (MMP-2) Regulates Astrocyte Motility in Conection with the Actin Cytoskeleton and Integrins” Glia 2006, 54, 272.
  • S. Hanessian, C. Gauchet, G. Charron, P. Nakache, “Design and Synthesis of Diversely Substituted Azacyclic Inhibitors of Endothelin Converting Enzyme”, J. Org. Chem. 2006, 71, 2760.
  • S. Hanessian, S. Guesné, Ludivine Riber, Julien Marin et al., "Targeting ACE and ECE with Dual Acting Inhibitors", Bioorg. Med. Chem. Lett. 2008, 18, 1058.
  • S. Hanessian; V. Babonneau; N. Boyer; C. Mannoury la Cour; M. J. Millan; G. DeNanteuil "Design and Synthesis of Potential Dual NK1/NK3 Receptor Antagonists" Bioorg. Med. Chem. Lett. 2014, 24, 510-514.
  • S. Hanessian; T. Jennequin, N. Boyer, V. Babonneau; U. Soma; C. Mannoury la Cour; M. J. Millan; G. DeNanteuil "Design, Synthesis and Pharmacological Characterization of Potent Dual NK1/NK3 Receptor Antagonists" ACS MedChem Lett 2014, 13, 550.
  • O. M. Saavedra; D. Karila; D. Brossard; A. Rojas; D. Dupuis, A. Gohier, C. Mannoury-Lacour; M.J .Millan; J.-C. Ortuno; S. Hanessian "Design and synthesis of novel N-sulfonyl-2-indoles that behave as 5HT6 ligands with significant selectivity for D3 over D2 receptors." Bioorg. Med. Chem. 2017, 25, 38-52
Neuraminidase, DNA Gyrase, HIV inhibitors (Flu, antibacterial, AIDS: Abbott Laboratories)
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  • S. Hanessian and P. Devasthale "Design and Synthesis of Novel, Pseudo C2 Symmetric Inhibitors of HIV Protease", Bioorg. Med. Chem. Lett. 1996, 6, 2201.
  • S. Hanessian, R. Saladino and J.C. Nunez, "On the Binding Site of Quinolone Antibacterials . An Attempt to Probe the Shen Model", Bioorg. Med. Chem. Lett. 1996, 6, 2333.
  • S. Hanessian and P.V. Devasthale, "Generation of Functional Diversity via Nitroaldol Condensations: A New and Stereocontrolled Route to Acyclic 1,3-Diamino-2-alcohols", Tetrahedron Lett. 1996, 37, 987.
  • S. Hanessian, J. Wang, D. Montgomery, V. Stoll, K. D. Stewart, W. Kati, C. Maring, D. Kempf, C. Hutchins and W. G. Laver, “Design, Synthesis, and Neuraminidase Inhibitory Activity of GS-4071 Analogs that Utilize a Novel Hydrophobic Paradigm”, Bioorg. Med. Chem. Lett. 2002, 12, 3425.
  • S. Hanessian, M. Bayrakdarian, and X. Luo “Total Synthesis of A-315675 – A Potent Inhibitor of Influenza Neuraminidase”, J. Am. Chem. Soc. 2002, 127, 4716.
Thrombin inhibitors (Cardiovascular: AstraZeneca, Sweden)
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  • S. Hanessian, E. Balaux, D. Musil, L.-L. Olsson, and I. Nilsson, “Exploring the Chiral Space within the Active Site α-Thrombin – Design, Synthesis and Inhibitory activity of a Constrained Mimic of D-Phe-Pro-Arg”, Bioorg. Med. Chem. Lett. 2000, 10, 243.
  • S. Hanessian, E. Therrien, K. Granberg, and I. Nilsson, “Targeting Thrombin and Factor VIIA – Design and Inhibitory Activity of Functionally Relevant Indolizidinones”, Bioorg. Med. Chem. Lett. 2002, 12, 2907.
  • S. Hanessian, R. Margarita, A. Hall, S. Johnstone, M. Tremblay, and L. Parlanti, “Total Synthesis and Structural Confirmation of the Marine Natural Product Dysinosin A – A Novel Inhibitor of Thrombin and Factor VIIa”, J. Am. Chem. Soc. 2002, 127, 13342.
  • S. Hanessian, W. van Otterlo, I. Nilsson, and U. Bauer, “Stereocontrolled Synthesis of a Prototype Library of Enantiopure 2,4-Disubstituted 4-Aryl 6-piperidones and Piperidines”, Tetrahedron Lett. 2002, 43, 1995.
  • S. Hanessian, R. Margarita, A. Hall, S. Johnstone, M. Tremblay, L. Parlanti, “New and old challenges in total synthesis. From concept to practice”, Pure Appl. Chem. 2003, 75, 209.
  • S. Hanessian, H. Sailes, and E. Therrien, “Synthesis of functionally diverse bicyclic sulfonamides as constrained proline analogues and application to the design of potential thrombin inhibitors”, Tetrahedron 2003, 59, 7047.
  • S. Hanessian and M. Tremblay, “The Aza-Prins Route to 1-Octahydroindoles: Total Synthesis and Structural Confirmation of the Antithrombotic Marine Natural Product Oscillarin”, J. Am. Chem. Soc. 2004, 126, 6604.
  • S. Hanessian, M. Tremblay, “Tandem Functionalization of Non-activated Alkenes and Alkynes in Intramolecular N-Acyloxyiminium Ion Carbocyclization. Synthesis of 6-Substituted Hydroindole 2-Carboxylic Acids”, Org. Lett. 2004, 6, 4683.
  • S. Hanessian, J. R. Del Valle, Y. Xue, N. Blomberg, “Total Synthesis and Structural Confirmation of Chlorodysinosin A”, J. Am. Chem. Soc. 2006, 128, 10491.
  • S. Hanessian, W. A .L .van Otterlo, M. Bayrakdarian, E. Therrien, I. Nilsson, J. Petersen, "Phenolic P2/P3 Core Motif as Thrombin Inhibitors - Design, Synthesis, and X-ray co-crystal structure" Bioorg. Med. Chem. Lett. 2006, 16, 1032.
  • K. Ersmark, S. Hanessian, “Structure-based Organic Synthesis of Unnatural Aeruginosin Hybrids as Potent Antithrombic Inhibitors”, Bioorg. Med. Chem. Lett. 2007, 17, 3480.
  • S. Hanessian, S. Guillemette, Karolina Ersmark, “P1, P3 Truncated Analogs of Oscillarin and their Inhibitory Activity against Blood Coagulation Factors”, Chimia 2007, 61, 361.
  • K. Ersmark, J. R. Del Valle, S. Hanessian, “Chemistry and Biology of the Aeruginosin Family of Serine Protease Inhibitors”, Angew Chem Int Ed. 2008, 47, 1202.
  • S. Hanessian, D. Simard, M. Bayrakdarian, E. Therrien, I. Nilsson, O. Fjellström, "Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs, Bioorg. Med. Chem. Lett. 2008, 18, 1972.
  • S. Hanessian, E. Therrien, W.van Otterlo, Y. Xue, D. Gustafsson, I. Nilsson, O. Fjellström, " From natural products to achiral drug prototypes: Potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs", Bioorg. Med. Chem. Lett. 2009, 19, 5429.
  • S. Hanessian, X. Wang, K. Ersmark, J. Del Valle, E. Klegraf, "Total Synthesis and Structural Revision of the Presumed Aeruginosins 205A and B", Org. Lett. 2009, 11, 4232.
  • S. Hanessian, A. Larsson, T. Fex, W. Knecht, N. Blomberg, "Design and Synthesis of Macrocyclic Indoles Targeting Blood Coagulation Cascade Factor Xia", Bioorg. Med. Chem. 2010, 20, 6925.
Renin inhibitors (Cardiovascular: ex. Ciba-Geigy, Basel, Process group)
​
  • S. Hanessian and R. Sadagopan, "Design and Synthesis of a Prototypical non-Peptidic Inhibitor Model for the Enzyme Renin", Bioorg. Med. Chem. Lett. 1994, 4, 1697.
  • S. Hanessian, T. Abad-Grillo, G. McNaughton-Smith, "Synthesis of (4S)-Hydroxymethyl-(2R)-(2-Propyl)-Butyrolactone: A Quest for a Practical Route to an Important Hydroxyethylene Isostere Chiron", Tetrahedron 1997, 53, 6281.
  • S. Hanessian, S. Claridge, and S. Johnstone, “The Power of Visual Imagery in Synthesis Planning – Stereocontrolled Approaches to CGP-60536B, a Potent Renin Inhibitor”, J. Org. Chem. 2002, 67, 4261.
  • S. Hanessian, S. Guesné, E. Chénard, "Total synthesis of "aliskiren": the first renin inhibitor in clinical practice for hypertension", Org. Lett. 2010, 12, 1816.
  • S. Hanessian; E. Chénard; S. Guesné; J. P. Cusson "Conception and Evolution of Stereocontrolled Strategies toward Functionalized 8-Aryloctanoic Acids Related to the Total Synthesis of Aliskiren" – J. Org. Chem. 2014, 79, 9531.
β-Lactams (Antibiotic: Lederle, Pearl River, N.Y; Glaxo-Verona, Italy; MethylGene, Dorval, P.Q.; Merck, Rahway; Roche, Nutley, N.J; Farmitalia, Milan)
​
  • S. Hanessian and M. Alpegiani, "Highly Chemoselective and Stereocontrolled Access to 6-α-allyl Penicillanates", Tetrahedron Lett. 1986, 27, 4857.
  • S. Hanessian and M. Alpegiani, "Highly Stereoselective Free Radical C-6-Allylation of Penams - Synthesis of a Novel β-Lactamase Inhibitor", Tetrahedron 1989, 45, 941.
  • S. Hanessian, D. Desilets and Y. L. Bennani, "A Novel Ring Closure Strategy for the Carbapenems: The Total Synthesis of (+)-Thienamycin", J. Org. Chem. 1990, 55, 3098..
  • S. Hanessian, K. Sumi and B. Vanasse, "The Stereocontrolled Synthesis of (2S,3R)-3-Alkyl-L-aspartic Acids Using a 2-Azetidinone Framework as a Chiral Template", Synlett 1992, 1, 33.
  • S. Hanessian, K. Sumi and R. Di Fabio, "The Stereocontrolled Synthesis of Versatile Carbapenem Intermediates Using the Barton O-Acyl 2-Thiopyridylhydroxamate Fragmentation", Tetrahedron Lett. 1992, 33, 749.
  • S. Hanessian, C. Couture, and N. Georgopapadakou, "Probing the Binding Domain of the Penicillin Side-chain Based on the Tipper-Strominger Hypothesis", Bioorg. Med. Chem. Lett. 1993, 3, 2323.
  • S. Hanessian and M. Rozema, "Synthesis and Biological Evaluation of 1-Substituted-7-1-Hydroxyethyl)Carbacephems - A Class of "Hybrid" Bicyclic β-Lactams", Bioorg. Med. Chem. Lett. 1994, 4, 2279.
  • S. Hanessian and G. B. Reddy, "Synthesis of Tricyclic β-Lactams - Functionally and Topologically Novel Carbacephems", Bioorg. Med. Chem. Lett. 1994, 4, 2285.
  • S. Hanessian, M. Rozema, G. B. Reddy, and J. Braganza, "Tricyclic β-lactams: Total Synthesis and Antibacterial Activity of 5β-Methoxy-Tribactam" Bio. Med. Chem. Lett. 1995, 5, 2535.
  • S. Hanessian and M. Rozema, "A Highly Stereoselective and Practical Total Synthesis of the Tricyclic β-Lactam Antibiotic GV104326 (4-Methoxy Trinem)", J. Am. Chem. Soc. 1996, 118, 9884.
  • S. Hanessian, A. M. Griffin and M. J. Rozema, “Tricyclic β-lactams: Total Synthesis and Antibacterial Activity of 5α-Methoxyethyl and 5α-hydroxyethyl Trinems” Bioorg. Med. Chem. Lett. 1997, 7, 1857.
  • S. Hanessian and B. Reddy, “Total Synthesis of Tricyclic β-lactams”, Tetrahedron 1999, 55, 3427.
  • S. Hanessian and R. Buckle, and M. Bayrakdarian “Design and Synthesis of a Novel Class of Constrained Tricyclic Pyrrolizidinone Carboxylic Acids as Carbapenem Mimics”, J. Org. Chem. 2002, 67, 3387.
Immunochemistry and Inflammation (Transplantation, pain, cancer: ex. Ciba-Geigy, Process group; Central research)
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  • S. Hanessian, D. Qiu, G.V. Reddy, H. Prabhanjan and B. Lou, "Synthesis of Clustered D-GalNac(TN) and D-Gal β(1-3) GalNac (T) Antigenic Motifs Using a Pentaerythritol Scaffold", Can. J. Chem. 1996, 74, 1738.
  • S. Hanessian, H. Prabhajan, D. Qiu and S. Nambiar, "The Synthesis of Chemically and Functionally Diverse Scaffolds from Pentaerytrhitol", Can. J. Chem. 1996, 74, 1731.
  • S. Hanessian, G.V. Reddy, H.K. Huynh, J. Pan, S. Pedatella, B. Ernst and H.C. Kolb, “Design and Synthesis of Sialyl Lex Mimetics Based on Carbocyclic Scaffolds Derived from (-)-Quinic Acid”, Bioorg. Med. Chem. Lett. 1997, 7, 2729.
  • S. Hanessian, H.K. Huynh, G.V. Reddy, G. McNaughton-Smith, B. Ernst and H.C. Kolb, - “Exploration of β-turn Scaffolding Motifs as Components of Sialyl LeX Mimetics and their Relevance to P-Selectin”, Bioorg. Med. Chem. Lett. 1998, 8, 2803.)
  • S. Hanessian, O. M. Saavedra, V. Mascitti and W. Marterer, “Practical Syntheses of B Disaccharide and Linear B Type 2 Trisaccharide - Non primate Epitope Markers Recognized by Human Anti α-Gal Antibodies During, Hyperacute Rejection of Xenotransplants” Tetrahedron 2001, 57, 3267.
  • S. Hanessian, H. K. Huynh, G. V. Reddy, and R. O. Duthaler, “Synthesis of Gal Determinant Epitopes, Their Glycomimetic Variants, and Trimeric Clusters – Relevance to Tumor Associated Antigens and to Discordant Xenografts”, Tetrahedron 2001, 57, 3281.
  • S. Hanessian, V. Mascitti, and O. Rogel, “Total Synthesis and a Potent Antagonist of E-Selectin”, J. Org. Chem. 2002, 67, 3346.
Natural products and mimetics (Osteoporosis, anthelmintics, analgesics: ex. Ciba-Agro, Basel; AstraZeneca, Sweden; Rhone-Poulenc Rorer, France; ex. Upjohn; Merck Rahway).
​
  • S. Hanessian, K. Sato, T.J. Liak, N. Danh, D. Dixit and B.V. Cheney, "Quantamycin" - A Computer-Simulated New-Generation Inhibitor of Bacterial Ribosomal Binding", J. Am. Chem. Soc. 1984, 106, 6114.
  • S. Hanessian, A. Ugolini, P.J. Hodges and D. Dubé, "The Controlled Degradation of Avermectin B1a", Tetrahedron Lett. 1986, 27, 2699.
  • S. Hanessian and B. Ronan, "Design and Synthesis of a Prototype Model Antagonist of Tachykinin NK-2 Receptor", Bioorg. Med. Chem. Lett. 1994, 4, 1397.
  • S. Hanessian, Q. Meng and E. Olivier, "An Unprecedented Ring Expansion in the Macrolide Series - Synthesis of Isobafilomycin A1", Tetrahedron Lett. 1994, 35, 5393.
  • S. Hanessian, A. Tehim, Q. Meng and K. Granberg, "A Remarkably Facile and Stereochemically Controlled Fragmentation Reaction in the Hygrolide Group of Macrolide Antibiotics", Tetrahedron Lett. 1996, 37, 9001.
  • S. Hanessian and M. Mauduit, “Highly Diastereoselective Intramolecular [1,2]-Stevens Rearrangements – Asymmetric Syntheses of Functionalized Isopavines as Morphinomimetics”, Angew. Chem. Int. Ed. 2001, 40, 3810.
  • S. Hanessian, J. Ma, W. Wang, and Y. Gai “Total Synthesis of Bafilomycin A1 Relying on Iterative 1,2-
  • Induction in Acyclic Precursors”, J. Am. Chem. Soc. 2001, 123, 10200.
  • S. Hanessian, M. Mauduit, E. Demont and C. Talbot, “Synthesis of Desymmetrized, Enantiopure Dihydro-Methano-Diarylazocines – Topologically Interesting Eyeteaser Molecules” Tetrahedron 2002, 58, 1485.
  • S. Hanessian, S. Parthasarathy, M. Mauduit, K. Payza, “The Power of Visual Imagery in Drug Design. Isopavines as a New Class of Morphinomimetics and Their Human Opioid Receptor Binding Activity.”, J. Med. Chem. 2003, 46, 34.
  • S. Hanessian, L. Zhan, R. Bovey, O. M. Saavedra, L. Juillerat-Jeanneret, “Functionalized Glycomers as Inhibitors of Human Glioblastoma Cell Growth”, J. Med. Chem. 2003, 46, 3600.
  • S. Hanessian, C. Talbot, P. Saravanan, “Diastereoselective [3,2]-Stevens and Sommelet-Hauser Rearrangements in the Dihydro-methanodibenzoazocine Series”, Synthesis 2006, Feature Article, 4, 723.
Histone deacetylase inhibitors (Sigma Tau, Pomezia, Italy)

  • S. Hanessian, V. Vinci, L. Auzzas, M. Marzi, G. Giannini, “Exploring alternative Zn-binding groups in the design of HDAC inhibitors: Squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA”, Bioorg. Med. Chem. Lett. 2006, 16, 4784.
  • S. Hanessian, L. Auzzas, G. Giannini, M. Marzi, W. Cabri, M. Barbarino, L. Vesci, C. Pisano, "ɷ-Alkoxy Analogues of SAHA (Vorinostat) as Inhibitors of HDAC. A Study of Chain-Length and Stereochemical Dependence, Bioorg. Med. Chem. Lett. 2007, 17, 6261.
  • S. Hanessian, L. Auzzas, A. Larsson, J. Zhang, G. Giannini, G. Gallo, A. Ciacci, W. Cabri, "Vorinostat-like Molecules as Structural, Stereochemical and Pharmacological Tools", ACS Med. Chem. Lett. 2010, 1, 70.
  • S. Hanessian, L. Auzzas, A. Larsson, R. Matera, A. Baraldi, G. Giannini, W. Cabri, G. Battistuzzi, G. Gallo, A. Ciacci, L. Vesci, C. Pisano, "Non-Natural Macrocyclic Inhibitors of Histone Deacetylase", J. Med. Chem. 2010, 53, 8387.

Nitric Oxide Synthase (NeurAxon, Toronto, Canada)
​
  • S. Hanessian; E. Stoffman; X. Mi, P. Renton, "Applications of Organocatalytic Asymmetric Synthesis to Drug Prototypes – Dual Action and Selective Inhibitors of n-Nitric Oxide Synthase", Org. Lett. 2011, 13, 840.