1,2,3-thiadiazole thioacetanilides. Part 2: Synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-yl]sulfanyl}acetanilides as HIV-1 inhibitors.
Chem Biodivers
; 7(7): 1717-27, 2010 Jul.
Article
en En
| MEDLINE
| ID: mdl-20658659
ABSTRACT
As part of our studies to discover new HIV-1 reverse transcriptase inhibitors, a series of 3,4-dichlorophenyl substituted 1,2,3-thiadiazole thioacetanilide (TTA=[(1,2,3-thiadiazole-5-yl)sulfanyl]acetanilide) derivatives were synthesized, and in vitro anti-HIV activity was evaluated. The results revealed that nearly half of the compounds show moderate-to-good inhibitory potency against HIV-1. In particular, compound 7f is highly potent, with an EC(50) value of 0.95+/-0.33 microM. The preliminary structure-activity relationship among the newly synthesized congeners is discussed.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tiadiazoles
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Infecciones por VIH
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VIH-1
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Fármacos Anti-VIH
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Acetanilidas
Límite:
Humans
Idioma:
En
Año:
2010
Tipo del documento:
Article