Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: The benzothiophene ring as an effective moiety

…, F Tramutola, F Berti, F Marino-Merlo

Index: Chiummiento, Lucia; Funicello, Maria; Lupattelli, Paolo; Tramutola, Francesco; Berti, Federico; Marino-Merlo, Francesca Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 8 p. 2948 - 2950

Full Text: HTML

Citation Number: 8

Abstract

Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating different heterocycles are described. The variation of heteroatom in such molecules has displayed totally different biological activities and a benzothiophene containing inhibitor has shown high potency against wild type HIV-1 protease with IC50= 60nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety.