title: Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: the benzothiophene ring as an effective moiety.
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.
authors.affiliation: Dipartimento di Chimica Antonio Mario Tamburro, Università degli Studi della Basilicata, Potenza, Italy.
authors.forename: Lucia
authors.initials: L
authors.lastname: Chiummiento
authors.forename: Maria
authors.initials: M
authors.lastname: Funicello
authors.forename: Paolo
authors.initials: P
authors.lastname: Lupattelli
authors.forename: Francesco
authors.initials: F
authors.lastname: Tramutola
authors.forename: Federico
authors.initials: F
authors.lastname: Berti
authors.forename: Francesca
authors.initials: F
authors.lastname: Marino-Merlo
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D006571:Heterocyclic Compounds; D013876:Thiophenes; C088015:benzothiophene