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Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.

Authors :
Miller JF
Andrews CW
Brieger M
Furfine ES
Hale MR
Hanlon MH
Hazen RJ
Kaldor I
McLean EW
Reynolds D
Sammond DM
Spaltenstein A
Tung R
Turner EM
Xu RX
Sherrill RG
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Apr 01; Vol. 16 (7), pp. 1788-94. Date of Electronic Publication: 2006 Feb 03.
Publication Year :
2006

Abstract

A novel series of P1 modified HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.

Details

Language :
English
ISSN :
0960-894X
Volume :
16
Issue :
7
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
16458505
Full Text :
https://doi.org/10.1016/j.bmcl.2006.01.035