Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: the benzothiophene ring as an effective moiety |
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Authors: | Chiummiento Lucia Funicello Maria Lupattelli Paolo Tramutola Francesco Berti Federico Marino-Merlo Francesca |
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Institution: | Dipartimento di Chimica Antonio Mario Tamburro, Università degli Studi della Basilicata, Potenza, Italy. |
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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 IC(50)=60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety. |
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