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Titolo:
A SERIES OF PENICILLIN DERIVED C2-SYMMETRICAL INHIBITORS OF HIV-1 PROTEINASE - SYNTHESIS, MODE OF INTERACTION, AND STRUCTURE-ACTIVITY-RELATIONSHIPS
Autore:
HUMBER DC; BAMFORD MJ; BETHELL RC; CAMMACK N; COBLEY K; EVANS DN; GRAY NM; HANN MM; ORR DC; SAUNDERS J; SHENOY BEV; STORER R; WEINGARTEN GG; WYATT PG;
Indirizzi:
GLAXO GRP RES LTD,DEPT MED CHEM GREENFORD UB6 0HE MIDDX ENGLAND GLAXO GRP RES LTD,DEPT VIROL GREENFORD UB6 0HE MIDDX ENGLAND GLAXO GRP RES LTD,DEPT DRUG METAB GREENFORD UB6 0HE MIDDX ENGLAND
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 21, volume: 36, anno: 1993,
pagine: 3120 - 3128
SICI:
0022-2623(1993)36:21<3120:ASOPDC>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEASE; TARGET; AIDS; CHROMATOGRAPHY; PURIFICATION; INFECTIVITY; PARTICLES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
D.C. Humber et al., "A SERIES OF PENICILLIN DERIVED C2-SYMMETRICAL INHIBITORS OF HIV-1 PROTEINASE - SYNTHESIS, MODE OF INTERACTION, AND STRUCTURE-ACTIVITY-RELATIONSHIPS", Journal of medicinal chemistry, 36(21), 1993, pp. 3120-3128

Abstract

The C2-symmetric diester 1 was identified by random screening as a novel inhibitor of HIV-1 proteinase. This led to the preparation of a series of related more potent amides from readily accessible penicillins. Many of the compounds showed potent antivirial activity in HIV-1-infected MT-4 cells and an ability to inhibit syncytia formation in infected C8166 cells, with no evidence of cytotoxicity. The compounds showed no activity against other aspartyl proteinases (renin, pepsin, and cathepsin D). Structure-activity relationships support a symmetrical interaction with the enzyme. Pharmacokinetic evaluation of the ethylamide 3 revealed it was subject to rapid plasma clearance and had low oralbioavailability.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 16/07/20 alle ore 05:45:13