Amino acid-based enantiomerically pure 3-substituted 1,4-benzodiazepin-2-ones: A new class of anti-ischemic agents

被引：45

作者：

Mishra, Jitendra Kumar

Garg, Puja

Dohare, Preeti

Kumar, Ashutosh

Siddiqi, Mohammad Imran

Ray, Madhur

Panda, Gautam ^{[1
]}

机构：

[1] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India

[2] Cent Drug Res Inst, Div Pharmacol, Lucknow 226001, Uttar Pradesh, India

[3] Cent Drug Res Inst, Mol & Struct Biol Div, Lucknow 226001, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期

关键词：

anti-ischemic agents; 1,4-benzodiazepin-2-ones; amino acids;

D O I：

10.1016/j.bmcl.2006.12.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1326 / 1331

页数：6

共 15 条

[1] Mechanisms for activation and antagonism of an AMPA-Sensitive glutamate receptor: Crystal structures of the GluR2 ligand binding core [J].