Amino acid-based enantiomerically pure 3-substituted 1,4-benzodiazepin-2-ones: a new class of anti-ischemic agents.
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.
Mishra
Jitendra Kumar
JK
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, UP, India.
Garg
Puja
P
Dohare
Preeti
P
Kumar
Ashutosh
A
Siddiqi
Mohammad Imran
MI
Ray
Madhur
M
Panda
Gautam
G
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
D000596:Amino Acids; D001570:Benzodiazepinones