Article
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.
Journal of medicinal chemistry - 27 Feb 2003
Ranise Angelo, Spallarossa Andrea, Schenone Silvia, Bruno Olga, Bondavalli Francesco, Vargiu Laura, Marceddu Tiziana, Mura Massimo, La Colla Paolo, Pani Alessandra
Abstract excerpt
A novel series of potent, selective HIV-1 N-acylthiocarbamate (ATC) nonnucleoside reverse transcriptase inhibitors (NNRTIs) is described. The title compounds were synthesized through a highly convergent, one-pot procedure. In cell-based assays, the lead compound (17c) prevented the HIV-1 multiplication with an EC(50) of 8 microM. The lead optimization strategy was developed by single or multiple modifications of...
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