Author/Authors :
Steven D. Young، نويسنده , , Muriel C. Amblard، نويسنده , , Susan F. Britcher، نويسنده , , Vanessa E. Grey، نويسنده , , Lee O. Tran، نويسنده , , William C. Lumma، نويسنده , , Joel R. Huff، نويسنده , , William A. Schleif، نويسنده , , Emilio E. Emini، نويسنده , , Julie A. OʹBrien، نويسنده , , Douglas J. Pettibone، نويسنده ,
Abstract :
A variety of 2-heterocycle substituted 3-phenysulfonyl-5-chloroindoles were investigated as replacements for the 2-carboxamide functionality of the potent HIV-1 reverse transcriptase inhibitor L-737, 126. The 2-carboxamide series of compounds typified by L-737,126 have poor solubility. Replacement of the carboxamide moiety with a variety of heterocycles results in a series of potent enzyme inhibitors with equivalent ex vivo antiviral activity and improved physicochemical properties.
