Abstract

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF NEW 1, 3, 4-THIADIAZOLE DERIVATIVES OF COUMARINS

Touseef Begum*, Khurshid I. Molvi, Suroor A. Kha

ABSTRACT

The new 7-[(5-{[(Z)-(substitutedphenyl)methylidene]amino}-1,3,4-thiadiazol-2-yl)methoxy]-4-methyl-2H-chromen-2-one Va–n have been synthesized from 7-[(5-amino-1,3,4-thiadiazol-2-yl)methoxy]-4-methyl-2H-chromen-2-one IV. All these compounds have been screened in-vivo for their anti-inflammatory and ulcerogenic activity. Compounds Vb, Vc, Vd and Vl were found to be potent member of this series, which showed 81.38%, 80.58%, 80.05% and 75.27% respectively, inflammation inhibitory activity at a dose of 20 mg kg−1 and 100 mg kg−1 p.o. after 1 hr; while the standard drug, indomethacin,
exhibited 66.34% anti-inflammatory activity at the same dose after 4hr. However, Compounds Vb, Vc ,Vd and Vl were found to be the most active and less ulcerogenic compound than the standard drug of this series. However, Compounds Vb, Vc, Vd, and Vl would be good candidates for lead molecules for anti-inflammatory activity with a larger margin of safety. The structures of these compounds have been established by FTIR, 1H-NMR, mass spectroscopic data and elemental analysis.

Keywords: Coumarins, Anti-inflammatory activity, Ulcerogenic activity, 1, 3, 4-thiadiazole, Quadrant, Craig plot.