Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents

被引：250
作者：
Barreca, ML
Chimirri, A
De Luca, L
Monforte, AM
Monforte, P
Rao, A
Zappalà, M
Balzarini, J
De Clercq, E
Pannecouque, C
Witvrouw, M
机构：
[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy
[2] Univ Magna Graecia Catanzaro, Dipartimento Sci Farmacobiol, I-88021 Roccelletta Di Borgia, CZ, Italy
[3] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 13期
关键词：
D O I：
10.1016/S0960-894X(01)00304-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Design, synthesis and anti-HIV activity of a series of 2,3-diaryl-1,3-thiazolidin-4-ones are reported. Some derivatives proved to be highly effective in inhibiting HIV-I replication at nanomolar concentrations thereby acting as non-nucleoside HIV-1 RT inhibitors (NNRTIs). SAR studies evidenced that the nature of the substituents at the 2 and 3 positions of the thiazolidinone nucleus largely influenced the in vitro anti-HIV activity of this new class of potent antiviral agents. (C) 2001 Elsevier Science Ltd. All rights reserved.
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页码：1793 / 1796
页数：4
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