新型基于吲哚的肌苷-5'-单磷酸脱氢酶抑制剂：在吲哚C-3位引入氢键受体
Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.
作者信息
Watterson Scott H, Dhar T G Murali, Ballentine Shelley K, Shen Zhongqi, Barrish Joel C, Cheney Daniel, Fleener Catherine A, Rouleau Katherine A, Townsend Robert, Hollenbaugh Diane L, Iwanowicz Edwin J
机构信息
Bristol-Myers Squibb PRI, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2003 Apr 7;13(7):1273-6. doi: 10.1016/s0960-894x(03)00109-4.
Abstract
The development of a series of novel indole-based inhibitors of 5'-inosine monophosphate dehydrogenase (IMPDH) is described. Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are outlined.
摘要
本文描述了一系列新型吲哚基5'-肌苷单磷酸脱氢酶（IMPDH）抑制剂的研发情况。对吲哚C-3位的各种氢键受体进行了探索。概述了体外研究得出的合成方法及构效关系（SAR）。
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