2-HETEROCYCLIC INDOLE-3-SULFONES AS INHIBITORS OF HIV-1 REVERSE-TRANSCRIPTASE

Authors
YOUNG SD AMBLARD MC BRITCHER SF GREY VE TRAN LO LUMMA WC HUFF JR SCHLEIF WA EMINI EE OBRIEN JA PETTIBONE DJ
Citation
Sd. Young et al., 2-HETEROCYCLIC INDOLE-3-SULFONES AS INHIBITORS OF HIV-1 REVERSE-TRANSCRIPTASE, Bioorganic & medicinal chemistry letters, 5(5), 1995, pp. 491-496
Citations number
14
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
5
Year of publication
1995
Pages
491 - 496
Database
ISI
SICI code
0960-894X(1995)5:5<491:2IAIOH>2.0.ZU;2-S
Abstract
A variety of 2-heterocycle substituted 3-phenysulfonyl-5-chloroindoles were investigated as replacements for the 7-carboxamide functionality of the potent HIV-L reverse transcriptase inhibitor L-737,126 The 2-c arboxamide series of compounds typified by L-737,126 have poor solubil ity. Replacement of the carboxamide moiety with a variety of heterocyc les results in a series of potent enzyme inhibitors with equivalent ex vivo antiviral activity and improved physicochemical properties.