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DESIGN AND SYNTHESIS OF A NEW CLASS OF POTENTIAL NON-PURINE XANTHINE OXIDASE INHIBITORS. Rajni Dhiman, Vikas Thakur, Charanjit kaur, Jagjeet singh, Sahil Sharma, Kunal Nepali, PMS Bedi

DESIGN AND SYNTHESIS OF A NEW CLASS OF POTENTIAL NON-PURINE XANTHINE OXIDASE INHIBITORS.

Rajni Dhiman, Vikas Thakur, Charanjit kaur, Jagjeet singh, Sahil Sharma, Kunal Nepali, PMS Bedi


International Journal of Natural Product Science 2012: Spl Issue 1:112.

Abstract(RBIP-112)

A rational approach for the design and synthesis of 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles as xanthine oxidase inhibitors (Fig.1) keeping in view the shape and structural features of 1 and 2 (Previously reported potent Xanthine oxidase inhibitors) .

Fifty three analogues of 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles were rationally designed, synthesized and evaluated for in vitro xanthine oxidase inhibitory activity using bovine milk xanthine oxidase (grade 1, ammonium sulfate suspension, Sigma–Aldrich) enzymatic assay as described in the literature1. Among the series of 53 compounds, compound 59 (Fig. 2) was found to be the most potent (IC50 = 5.30 µM) comparable to that of allopurinol (IC50 = 8.3 µM). Docking studies were also performed and it was found that the S-isomer fits well in the Xanthine Oxidase Binding cavity (Fig. 3). On the basis of SAR studies, a basic pharmacophore with the structural features required for Xanthine Oxidase inhibitory activity has been proposed (Fig. 4).
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