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|Title:||S-triazolyl .alpha.-mercapto acetanilides as inhibitors of HIV reverse transcriptase|
|Abstract:||A series of S-triazolyl .alpha.-mercaptoacetanilides having general structure (1) are provided, where Q is CO.sub.2H, CONR.sub.2, SO.sub.3H, or SO.sub.2NR.sub.2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections. ##STR00001##|
|Inventor(s):||Girardet; Jean-Luc (San Diego, CA), Koh; Yung Hyo (Irvine, CA), De La Rosa; Martha (San Diego, CA), Gunic; Esmir (San Diego, CA), Hong; Zhi (Irvine, CA), Lang; Stanley (Laguna Niguel, CA), Kim; Hong Woo (San Diego, CA)|
|Assignee:||Ardea Biosciences, Inc. (San Diego, CA)|
|Filing Date:||Jun 30, 2011|
|Claims:||1. A compound of Formula A'' ##STR00326## wherein R.sup.1 is C.sub.1-3 alkyl, CF.sub.3, CHF.sub.2, CH.sub.2F, Cl, Br, NH.sub.2, or hydrogen; R.sup.2 is 4-Q-naphth-1-yl or 4-Q-phen-1-yl; Q is C.sub.2-5 alkyl; W is S, O or an optionally substituted amine; R.sup.3 is C.sub.1-3 alkyl, CF.sub.3, CHF.sub.2, CH.sub.2F, Cl, Br; and R.sup.4 is COR' or S(O).sub.2R', wherein R' is NH.sub.2 or NH(alkyl). |
2. The compound of claim 1, where W is S.
3. The compound of claim 1, wherein R.sup.1 is other than H.
4. The compound of claim 1, wherein Q is ethyl.
5. The compound of claim 1, wherein R.sup.3 is chloro or methyl.
6. The compound of claim 1, which is 2-[5-bromo-4-(4-ethyl-naphthalen-1-yl)-4H-[1,2,4]triazol-3-ylsulfanyl]-N-- (2-chloro-4-sulfamoyl-phenyl)-acetamide or 2-[5-bromo-4-(4-ethyl-naphthalen-1-yl)-4H-[1,2,4]triazol-3-ylsulfanyl]-N-- (2-chloro-4-carbamoyl-phenyl)-acetamide.