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

Abstract：

:A novel series of 1,2,3-thiadiazole thioacetanilide (TTA) derivatives have been designed, synthesized and evaluated for its anti-HIV activities in MT-4 cells. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations. Among them, 2-[4-(2,4-dichlorophenyl)-1,2,3-thiadiazol-5-ylthio]-N-(2-nitrophenyl)acetamide 7d2 was identified as the most promising compound (EC(50)=0.059+/-0.02 microM, CC(50)>283.25 microM, SI>4883). The structure-activity relationship (SAR) of these novel structural congeners is discussed.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhan P,Liu X,Cao Y,Wang Y,Pannecouque C,De Clercq E

doi

10.1016/j.bmcl.2008.09.055

subject

Has Abstract

pub_date

2008-10-15 00:00:00

pages

5368-71

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01125-6

journal_volume

18

pub_type

杂志文章

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