2-Heterocyclic Indole-3-Sulfones As Inhibitors Of Hiv-1 Reverse-Transcriptase

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-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.