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 = 60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety.
Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: The benzothiophene ring as an effective moiety / Lucia, Chiummiento; Maria, Funicello; Paolo, Lupattelli; Francesco, Tramutola; Berti, Federico; Francesca Marino, Merlo. - In: BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS. - ISSN 1464-3405. - STAMPA. - 22:(2012), pp. 2948-2950. [10.1016/j.bmcl.2012.02.046]
Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: The benzothiophene ring as an effective moiety
BERTI, FEDERICO;
2012-01-01
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 = 60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety.Pubblicazioni consigliate
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