Microwave-assisted synthesis and anti-YFV activity of 2,3-diaryl-1,3-thiazolidin-4-ones

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Purpose:
The purpose of this study was to prepare several 1,3-thaizolidin-4-ones bearing variously substituted diaryl ring at C-2 and N-3 positions and evaluate them for their anti-YFV activity.

Methods:
Several 1,3-thaizolidin-4-ones were prepared by reacting substituted benzaldehyde with equimolar amount of an appropriate substituted aromatic amine in the presence of an excess of mercaptoacetic acid in toluene utilizing microwave irradiation. The synthesized compounds were also evaluated for their inhibitory effects on the replication of YFV in green monkey kidney (Vero) cells (ATCC CCL81), by means of a cytopathic effect reduction assay. Results: The compound DS1 emerged as the most potent anti-YFV agent with EC50 of 6.9 µM and CC50 more than 100 µM making it more potent than ribavirin. Conclusion: 2,3-diaryl-1,3-thiazolidin-4-ones possess anti-YFV potency.

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Author(s): 
Dharmarajan Sriram, Perumal Yogeeswari, TG Ashok Kumar.
Journal: 
J Pharm Pharmaceut Sci (www.cspscanada.org) 8(3) September - December 2005
Copyright: 
Canadian Society for Pharmaceutical Sciences