Résumé
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.
A variety of indole-2-heterocycles were investigated as replacements for the 2-carboxamide of the HIV-1 RT inhibitor L-737,126. Replacement of the carboxamide moiety with a variety of heterocycles results in a series of potent enzyme inhibitors with excellent
ex vivo antiviral activity.