Mishra Jitendra Kumar, Garg Puja, Dohare Preeti, Kumar Ashutosh, Siddiqi Mohammad Imran, Ray Madhur, Panda Gautam
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, UP, India.
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1326-31. doi: 10.1016/j.bmcl.2006.12.001. Epub 2006 Dec 3.
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.
对一系列源自S型和R型氨基酸的3-取代-1,4-苯二氮䓬-2-酮进行了体外抗缺血活性评估。用化合物7h、16、9d和17处理可减少凋亡神经元数量，但增加神经元活力。减少凋亡的化合物可保护神经元免受缺血性损伤。基于分子模型研究对源自S型和R型氨基酸的1,4-苯二氮䓬-2-酮活性差异进行了讨论和解释。
