Synthesis and biological evaluation of 2,3-diaryl substituted-1,3-thiazolidin-4-ones as anti-HIV agents.
Med Chem
; 3(4): 355-63, 2007 Jul.
Article
de En
| MEDLINE
| ID: mdl-17627572
ABSTRACT
A series of 1,3-thiazolidin-4-ones and metathiazanones were synthesized and evaluated as anti-HIV agents. The results of the in vitro assays showed that some of the synthesized compounds were effective inhibitor of reverse transcriptase enzyme of human immunodeficiency virus type-1 (HIV-1) at micromolar concentrations with less cytotoxicity in MT-4 cells as compared to thiazolobenzimidazole (TBZ). Structure-activity relationship studies revealed that the nature of the substituents at the 2 and 3 positions of the thiazolidin-4-one nucleus had a significant impact on the in vitro anti-HIV activity of this class of antiretroviral agents. One of the compounds, 1, inhibited the enzyme at 0.204 microM concentrations with minimal cytotoxicity to MT-4 cells.
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Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Agents antiVIH
/
Thiazolidines
Limites:
Humans
Langue:
En
Journal:
Med Chem
Sujet du journal:
QUIMICA
Année:
2007
Type de document:
Article
Pays d'affiliation:
Inde