John E Leet

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. ncbi request reprint Nocathiacins, new thiazolyl peptide antibiotics from Nocardia sp. II. Isolation, characterization, and structure determination
    John E Leet
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Antibiot (Tokyo) 56:232-42. 2003
  2. pmc Cytotoxic xanthones from Psorospermum molluscum from the Madagascar rain forest
    John E Leet
    Bristol Myers Squibb Company, Wallingford, Connecticut 06492, USA
    J Nat Prod 71:460-3. 2008
  3. doi request reprint N-Demethylation of nocathiacin I via photo-oxidation
    Wenying Li
    Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 18:4051-3. 2008
  4. doi request reprint Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation
    Xiaoliang Zhuo
    Departments of Biotransformation, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA
    Drug Metab Dispos 38:5-15. 2010
  5. ncbi request reprint Chemical conversion of nocathiacin I to nocathiacin II and a lactone analogue of glycothiohexide alpha
    Timothy P Connolly
    Pharmaceutical Research Institute, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Nat Prod 68:550-3. 2005
  6. ncbi request reprint Nocathiacins, new thiazolyl peptide antibiotics from Nocardia sp. I. Taxonomy, fermentation and biological activities
    Wenying Li
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Antibiot (Tokyo) 56:226-31. 2003
  7. ncbi request reprint Observation of O-H...N scalar coupling across a hydrogen bond in nocathiacin I
    Xiaohua Stella Huang
    Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06942, USA
    Magn Reson Chem 45:447-50. 2007
  8. ncbi request reprint Synthesis of novel nocathiacin-class antibiotics. Condensation of glycolaldehyde with primary amides and tandem reductive amination of amadori-rearranged 2-oxoethyl intermediates
    Peter Hrnciar
    Bristol Myers Squibb Co, Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Org Chem 67:8789-93. 2002
  9. ncbi request reprint Conformation and absolute configuration of nocathiacin I determined by NMR spectroscopy and chiral capillary electrophoresis
    Keith L Constantine
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    J Am Chem Soc 124:7284-5. 2002
  10. ncbi request reprint Donepezil primarily attenuates scopolamine-induced deficits in psychomotor function, with moderate effects on simple conditioning and attention, and small effects on working memory and spatial mapping
    Mark D Lindner
    Department 401, Neuroscience Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA
    Psychopharmacology (Berl) 188:629-40. 2006

Detail Information

Publications18

  1. ncbi request reprint Nocathiacins, new thiazolyl peptide antibiotics from Nocardia sp. II. Isolation, characterization, and structure determination
    John E Leet
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Antibiot (Tokyo) 56:232-42. 2003
    ..The structures of nocathiacins I-III were determined by spectroscopic (2D-NMR, MSn) methods, and share structural similarities to glycothiohexide-alpha (4)...
  2. pmc Cytotoxic xanthones from Psorospermum molluscum from the Madagascar rain forest
    John E Leet
    Bristol Myers Squibb Company, Wallingford, Connecticut 06492, USA
    J Nat Prod 71:460-3. 2008
    ..A new hydroxyprenylated xanthone ( 5) is also described. Xanthones 1 and 4 showed selective in vitro cytotoxicity against ABAE cells (bovine endothelial cell line)...
  3. doi request reprint N-Demethylation of nocathiacin I via photo-oxidation
    Wenying Li
    Bristol Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 18:4051-3. 2008
    ..Irradiation of 1 in DMF/CH(2)Cl(2) with UV light of 380 nm led to a cyclic product 2, which was hydrolyzed to yield the desired nocathiacin VI (3). Treatment of 1 with shorter UV light caused trans-cis isomerization of a c-c double bond...
  4. doi request reprint Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation
    Xiaoliang Zhuo
    Departments of Biotransformation, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA
    Drug Metab Dispos 38:5-15. 2010
    ....
  5. ncbi request reprint Chemical conversion of nocathiacin I to nocathiacin II and a lactone analogue of glycothiohexide alpha
    Timothy P Connolly
    Pharmaceutical Research Institute, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Nat Prod 68:550-3. 2005
    ..In contrast to glycothiohexide alpha (3), this lactone analogue (5) was found to exhibit in vivo antibacterial efficacy in an animal (mouse) infection model...
  6. ncbi request reprint Nocathiacins, new thiazolyl peptide antibiotics from Nocardia sp. I. Taxonomy, fermentation and biological activities
    Wenying Li
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Antibiot (Tokyo) 56:226-31. 2003
    ....
  7. ncbi request reprint Observation of O-H...N scalar coupling across a hydrogen bond in nocathiacin I
    Xiaohua Stella Huang
    Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06942, USA
    Magn Reson Chem 45:447-50. 2007
    ..This observation provides valuable information for characterizing molecular conformations, and for studying structure-activity relationships...
  8. ncbi request reprint Synthesis of novel nocathiacin-class antibiotics. Condensation of glycolaldehyde with primary amides and tandem reductive amination of amadori-rearranged 2-oxoethyl intermediates
    Peter Hrnciar
    Bristol Myers Squibb Co, Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    J Org Chem 67:8789-93. 2002
    ..This transformation readily tolerates the complex architecture of nocathiacins and allows selective incorporation of water solubilizing groups to the primary amide in 2 without protecting group manipulation...
  9. ncbi request reprint Conformation and absolute configuration of nocathiacin I determined by NMR spectroscopy and chiral capillary electrophoresis
    Keith L Constantine
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    J Am Chem Soc 124:7284-5. 2002
    ..The single threonine residue in nocathiacin I was subsequently determined to be l-threonine by chiral capillary electrophoresis, allowing the absolute configurations of all 10 chiral centers to be defined...
  10. ncbi request reprint Donepezil primarily attenuates scopolamine-induced deficits in psychomotor function, with moderate effects on simple conditioning and attention, and small effects on working memory and spatial mapping
    Mark D Lindner
    Department 401, Neuroscience Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA
    Psychopharmacology (Berl) 188:629-40. 2006
    ....
  11. ncbi request reprint Adverse effects of gabapentin and lack of anti-allodynic efficacy of amitriptyline in the streptozotocin model of painful diabetic neuropathy
    Mark D Lindner
    Department of Neuroscience Biology, Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA
    Exp Clin Psychopharmacol 14:42-51. 2006
    ..These findings challenge the consensus opinions about these primary treatments for PDN and suggest that their therapeutic and adverse effects should be explored further in pain patients...
  12. doi request reprint Biotransformation of Daclatasvir In Vitro and in Nonclinical Species: Formation of the Main Metabolite by Pyrrolidine δ-Oxidation and Rearrangement
    Wenying Li
    Departments of Pharmaceutical Candidate Optimization W L, W Z, X L, X H, R M F, J C C, S Y C, L M, M Z, Y Z S, W G H, B M J, Synthesis and Analysis Technology Team J E L, Virology M G, and Chemistry O D L, V N, J G, J E, Y H, M B, L G H, Bristol Myers Squibb Company, Wallingford, Connecticut
    Drug Metab Dispos 44:809-20. 2016
    ..This biotransformation profile supported the continued development of daclatasvir, which is now marketed for the treatment of chronic hepatitis C virus infection. ..
  13. doi request reprint Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey
    Benjamin M Johnson
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA
    Drug Metab Dispos 36:2475-83. 2008
    ....
  14. doi request reprint Labware additives identified to be selective monoamine oxidase-B inhibitors
    Jeremy Stewart
    Leads Discovery and Optimization, Research and Development, Bristol Myers Squibb Co, Wallingford, CT, USA
    J Biomol Screen 19:1409-14. 2014
    ....
  15. doi request reprint Extraction, identification, and functional characterization of a bioactive substance from automated compound-handling plastic tips
    John Watson
    Bristol Myers Squibb Company, Research and Development, Wallingford, Connecticut 06492, USA
    J Biomol Screen 14:566-72. 2009
    ..These contaminants may further possess biological activity and are therefore a potential source of assay-specific confounding artifacts...
  16. doi request reprint Best practices in compound management for preserving compound integrity and accurately providing samples for assays
    Sandra L Matson
    Department of Applied Biotechnologies, Bristol Myers Squibb, Wallingford, Connecticut 06492, USA
    J Biomol Screen 14:476-84. 2009
    ..This article presents the results of these experiments and how they affect compound integrity and the accuracy of compound management processes...
  17. pmc Discovery of potent hepatitis C virus NS5A inhibitors with dimeric structures
    Julie A Lemm
    Department of Virology, Bristol Myers Squibb Research, 5 Research Parkway, Wallingford, Connecticut 06492, USA
    Antimicrob Agents Chemother 55:3795-802. 2011
    ..This culminated in the identification of BMS-790052, a compound that preserves the symmetry discovered with BMS-346...
  18. doi request reprint HPLC biogram analysis: a powerful tool used for hit confirmation in early drug discovery
    John E Leet
    Bristol Myers Squibb Company, Wallingford, CT, USA
    J Biomol Screen 20:681-7. 2015
    ..Biograms are employed to track, isolate, and identify the source of biological activity in such samples, often yielding important information for program decisions. ..