Literature

Abstract

A series of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)acetamide (TTA) derivatives were synthesized and evaluated as potent inhibitors of HIV-1. Among the newly disclosed TTAs, compounds 7f, 7 g and 7c were the most potent inhibitors of HIV-1 replication of the series (EC(50)=0.17+/-0.02, 0.36+/-0.19 and 0.39+/-0.05 microM, respectively), coupled with a reasonable selectivity index (SI>1452, >845, and >774, respectively). They possess improved or similar HIV-1 inhibitory activity compared with NVP (EC(50)=0.208 microM) and DLV (EC(50)=0.320 microM). The preliminary structure-activity relationships among the newly synthesized congeners are discussed briefly and rationalized by docking studies.

DOI： 10.1016/j.ejmech.2009.06.037

Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

European Journal of Medicinal Chemistry 2009.0

1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors

Bioorganic & Medicinal Chemistry Letters 2008.0

Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs)

Bioorganic & Medicinal Chemistry 2008.0

Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

Bioorganic & Medicinal Chemistry 2009.0

Synthesis and anti-HIV activity evaluation of novel N′-arylidene-2-[1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio]acetohydrazides

Medicinal Chemistry Research 2010.0

Thiadiazole Derivatives: Highly Potent and Specific HIV-1 Reverse Transcriptase Inhibitors