Design and synthesis of novel conformationally restricted HIV protease inhibitors

Design and synthesis of novel conformationally restricted HIV protease inhibitors
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DOI:
10.1016/s0960-894x(98)00670-2
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发表时间:
1998-12-15
影响因子:
2.7
通讯作者:
Tung, RD
Tung, RD
中科院分区:
医学4区
文献类型:
--
作者:
Salituro, FG;Baker, CT;Tung, RD

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先前已经描述了以化合物2为代表的一组HIV蛋白酶抑制剂。该化合物的结构和构象分析表明,分子 P-1/P-2 部分的构象限制可能会产生一组新型的有效蛋白酶抑制剂。因此,探针化合物3-7被设计、合成并被发现是HIV蛋白酶的有效抑制剂。 (C) 1998 Elsevier Science Ltd. 保留所有权利。
A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested that conformational restriction of the P-1/P-2 portion of the molecule could lead to a novel set of potent protease inhibitors. Thus, probe compounds 3-7 were designed, synthesized, and found to be potent inhibitors of HIV protease. (C) 1998 Elsevier Science Ltd. All rights reserved.