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Titolo:
Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a] benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors
Autore:
Chimirri, A; Grasso, S; Monforte, P; Rao, A; Zappala, M; Monforte, AM; Pannecouque, C; Witvrouw, M; Balzarini, J; De Clercq, E;
Indirizzi:
Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy Univ Messina Messina Italy I-98168 o Farmacochim, I-98168 Messina, Italy Univ Catanzaro, Fac Farm, I-88021 Roccelletta Di Borgia, CZ, Italy Univ Catanzaro Roccelletta Di Borgia CZ Italy I-88021 i Borgia, CZ, Italy Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Leuven, Belgium Katholieke Univ Leuven Leuven Belgium B-3000 Res, B-3000 Leuven, Belgium
Titolo Testata:
ANTIVIRAL CHEMISTRY & CHEMOTHERAPY
fascicolo: 4, volume: 10, anno: 1999,
pagine: 211 - 217
SICI:
0956-3202(199907)10:4<211:SABAON>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTI-HIV AGENTS; NONNUCLEOSIDE INHIBITORS; MECHANISM;
Keywords:
1H,3H-thiazolo[3,4-a]benzimidazoles; TBZs; anti-HIV activity; NNRTIs;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
16
Recensione:
Indirizzi per estratti:
Indirizzo: Monforte, P Univ Messina, Dipartimento Farmacochim, Viale Annunziata, I-98168 Messina,Italy Univ Messina Viale Annunziata Messina Italy I-98168 ina,Italy
Citazione:
A. Chimirri et al., "Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a] benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors", ANTIVIR CHE, 10(4), 1999, pp. 211-217

Abstract

Using a known human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitor (NNRTI), 1-(2.6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole (TBZ NSC 625487) as the lead structure for drug design, a series of novel 1H,3H-thiazolo[3,4-a]benzimidazole derivatives substituted on the benzene-fused ring was prepared. Their in vitro anti-HIV-1 activity, as well as their inhibitory effects on the viral reverse transcriptase, were evaluated. The structure-activity relationships for these compounds are described and the results suggest that the apolar binding pocket of RT, into which the NNRTIs must fit, can accommodate only groups with a limited size and shape.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 15:11:41