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新型2-咪唑啉酮和四氢嘧啶-2(1H)-酮作为潜在TACE抑制剂的研究：设计、合成、分子模拟及初步生物学评价

Studies on novel 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones as potential TACE inhibitors: design, synthesis, molecular modeling, and preliminary biological evaluation.

作者信息

DasGupta Shirshendu, Murumkar Prashant R, Giridhar Rajani, Yadav Mange Ram

机构信息

Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara 390 001, Gujarat, India.

出版信息

Bioorg Med Chem. 2009 May 15;17(10):3604-17. doi: 10.1016/j.bmc.2009.04.003. Epub 2009 Apr 8.

DOI:10.1016/j.bmc.2009.04.003
PMID:19394232
Abstract

Compounds belonging to the class of 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones were synthesized and evaluated for their TACE inhibitory activity. Most of the compounds showed very good TACE inhibitory activity. Docking study clearly indicates importance of the P1' group of the inhibitor for the TACE inhibitory activity. This work proves that these two classes of molecules could be used as potential leads for the development of TACE inhibitors.

摘要

合成了属于2-咪唑啉酮类和四氢嘧啶-2(1H)-酮类的化合物，并对其TACE抑制活性进行了评估。大多数化合物表现出非常好的TACE抑制活性。对接研究清楚地表明了抑制剂的P1'基团对TACE抑制活性的重要性。这项工作证明这两类分子可作为开发TACE抑制剂的潜在先导化合物。

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