Quinolone-based IMPDH inhibitors: Introduction of basic residues on ring D and SAR of the corresponding mono, Di and Benzofused analogues
Quinolone-based IMPDH inhibitors: Introduction of basic residues on ring D and SAR of the corresponding mono, Di and Benzofused analogues
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DOI：
10.1016/s0960-894x(02)00945-9
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发表时间：
2003-02-10
影响因子：
2.7
通讯作者：
Iwanowicz, EJ
中科院分区：
文献类型：
--
作者：
Dhar, TGM;Watterson, SH;Iwanowicz, EJ
描述了在基于喹诺酮的IMPDH抑制剂D环上引入碱性残基而衍生的类似物的合成和结构-活性关系（SAR）。这导致鉴定出化合物27为IMPDH的有效抑制剂，其水溶性比先导化合物1显著改善。(C)2002爱思唯尔科技有限公司版权所有。
The synthesis and the structure-activity relationships (SAR) of analogues derived from the introduction of basic residues on ring D of quinolone based inhibitors of IMPDH are described. This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1. (C) 2002 Elsevier Science Ltd. All rights reserved.