Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents.
作者信息
Barreca M L, Chimirri A, De Luca L, Monforte A M, Monforte P, Rao A, Zappalà M, Balzarini J, De Clercq E, Pannecouque C, Witvrouw M
机构信息
Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168, Messina, Italy.
出版信息
Bioorg Med Chem Lett. 2001 Jul 9;11(13):1793-6. doi: 10.1016/s0960-894x(01)00304-3.
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-1 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.
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