Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Parallel synthesis, molecular modelling and structure–activity relationship studies on …

…, A Spallarossa, A Ranise, P Fossa, P La Colla…

Index: Cesarini, Sara; Spallarossa, Andrea; Ranise, Angelo; Fossa, Paola; Colla, Paolo La; Sanna, Giuseppina; Collu, Gabriella; Loddo, Roberta Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 7 p. 4160 - 4172

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Citation Number: 14

Abstract

In order to expand the structure–activity relationship (SAR) studies on Thiocarbamates (TCs), a recently discovered class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors, 38 analogues of the lead O-[2-(2-pyridyl) ethyl]-N-phenylthiocarbamate 1 were prepared by parallel solution-phase synthesis. The SAR strategy was focused on the variation (mono-and disubstitution) of the N-phenyl ring and the replacement of the 2- ...