Novel inhibitors of HIV protease: Design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds
Novel inhibitors of HIV protease: Design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds
复制标题
DOI：
10.1016/s0960-894x(00)00163-3
复制
发表时间：
2000-06-05
影响因子：
2.7
通讯作者：
Wright, LL
中科院分区：
文献类型：
--
作者：
Spaltenstein, A;Almond, MR;Wright, LL
合成了一系列新型的含有环状P1/P2骨架的HIV蛋白酶抑制剂，并对其生物活性进行了评价。反式3，5-二苄基-2-氧代吡咯烷酮环系统在与茚满醇胺衍生的P ′-骨架结合时，在体外产生50 pM的抗HIV蛋白酶的酶抑制剂。该化合物在基于MT-4细胞的抗病毒试验中也显示出与目前市售药物相当的活性。(C)2000爱思唯尔科技有限公司版权所有。
A novel series of HIV protease inhibitors containing cyclic P1/P2 scaffolds has been synthesized and evaluated for biological activity. The trans 3,5-dibenzyl-2-oxo pyrrolidinone ring system resulted in a 50 pM enzyme inhibitor against HIV protease in vitro when combined with an indanolamine derived P'-backbone. This compound also shows comparable activity to currently marketed drugs in the MT-4 cell-based antiviral assay. (C) 2000 Elsevier Science Ltd. All rights reserved.