Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2P3 moieties
Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2P3 moieties
复制标题
DOI：
10.1016/j.bmcl.2007.05.039
复制
发表时间：
2007-08-01
影响因子：
2.7
通讯作者：
Kiso, Yoshiaki
中科院分区：
文献类型：
--
作者：
Ami, Ei'ichi;Nakahara, Koichiro;Kiso, Yoshiaki
我们根据临床候选药物KNI-764的结构，设计了几种具有不同D-半胱氨酸衍生物作为P-2/P-3部分的HIV蛋白酶抑制剂。在此，我们报告了它们的合成，HIV蛋白酶抑制活性，HIV 11113细胞抑制活性，细胞毒性和对耐药HIV菌株的抑制活性。KNI-1931对HIV蛋白酶表现出明显的选择性，对耐药菌株表现出高效力，超过了利托那韦和奈非那韦。(c)2007爱思唯尔有限公司版权所有。
We designed several HIV protease inhibitors with various D-cysteine derivatives as P-2/P-3 moieties based on the structure of clinical drug candidate, KNI-764. Herein, we report their synthesis, HIV protease inhibitory activity, HIV 11113 cell inhibitory activity, cellular toxicity, and inhibitory activity against drug-resistant HIV strains. KNI-1931 showed distinct selectivity against HIV proteases and high potency against drug-resistant strains, surpassing those of Ritonavir and Nelfinavir. (c) 2007 Elsevier Ltd. All rights reserved.