Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite
Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite
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DOI：
10.1016/j.bmcl.2006.10.084
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发表时间：
2007-02-01
影响因子：
2.7
通讯作者：
Mitsuya, Hiroaki
中科院分区：
文献类型：
--
作者：
Nishizawa, Rena;Nishiyama, Toshihiko;Mitsuya, Hiroaki
基于氧化代谢产物的信息，设计合成了羟基化衍生物。与非羟基化衍生物和其它异构体相比，衍生自β-取代的（2 R，3R）-2-氨基-3-羟基丙酸的化合物显示出改善的对MIP-1 α与人CCR 5结合的抑制活性。(c)2006爱思唯尔有限公司版权所有。
Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from beta-substituted (2R,3R)-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of MIP-1 alpha to human CCR5, compared with the non-hydroxylated derivatives and the other isomers. (c) 2006 Elsevier Ltd. All rights reserved.