Microwave-assisted synthesis and anti-YFV activity of 2,3-diaryl-1,3-thiazolidin-4-ones.
OBJECTIVE
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 microM and CC50 more than 100 microM making it more potent than ribavirin.


CONCLUSIONS
2,3-diaryl-1,3-thiazolidin-4-ones possess anti-YFV potency.
Sriram
Dharmarajan
D
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani, India. dsriram@bits-pilani.ac.in
Yogeeswari
Perumal
P
Kumar
T G Ashok
TG
D000818:Animals; D002522:Chlorocebus aethiops; D008872:Microwaves; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014709:Vero Cells; D015005:Yellow fever virus / Q000187:drug effects* / Q000502:physiology
D013844:Thiazoles