title: Amino acid-based enantiomerically pure 3-substituted 1,4-benzodiazepin-2-ones: a new class of anti-ischemic agents.
abstract: A series of 3-substituted 1,4-benzodiazepin-2-ones derived from S and R amino acids were evaluated for their anti-ischemic activity in vitro. Treatment with compounds 7h, 16, 9d, and 17 decreased the apoptotic neuronal number, however increased the neuronal viability. The compounds decreasing apoptosis could protect neurons from the ischemic injury. The difference in the activities of 1,4-benzodiazepin-2-ones derived from S- and R-amino acids is discussed and explained on the basis of molecular modeling studies.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, UP, India.
authors.forename: Jitendra Kumar
authors.initials: JK
authors.lastname: Mishra
authors.forename: Puja
authors.initials: P
authors.lastname: Garg
authors.forename: Preeti
authors.initials: P
authors.lastname: Dohare
authors.forename: Ashutosh
authors.initials: A
authors.lastname: Kumar
authors.forename: Mohammad Imran
authors.initials: MI
authors.lastname: Siddiqi
authors.forename: Madhur
authors.initials: M
authors.lastname: Ray
authors.forename: Gautam
authors.initials: G
authors.lastname: Panda
mesh_terms: D000596:Amino Acids; D017209:Apoptosis / Q000187:drug effects; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D001665:Binding Sites; D002470:Cell Survival / Q000187:drug effects; D005434:Flow Cytometry; D006801:Humans; D007511:Ischemia / Q000188:drug therapy* / Q000517:prevention & control; D008958:Models, Molecular; D009474:Neurons / Q000187:drug effects / Q000473:pathology; D011485:Protein Binding; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D001570:Benzodiazepinones