Beta-N-cyanoethyl acyl hydrazide derivatives: a new class of beta-glucuronidase inhibitors |
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Authors: | Khan Khalid Mohammed Shujaat Shahida Rahat Shagufta Hayat Safdar Atta-ur-Rahman Choudhary Muhammad Iqbal |
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Institution: | H.E.J. Research Institute of Chemistry, International Centre for Chemical Sciences, University of Karachi, Pakistan. hasaan2@super.net.pk |
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Abstract: | Eight new beta-N-substituted acyl hydrazides along with their corresponding acyl derivatives were synthesized and screened for in vitro beta-glucuronidase inhibition and found to be active against the enzyme. All of these compounds were found to be noncompetitive inhibitors except for N'-(2-cyanoethyl)-4-hydroxy benzohydrazide (10), which was found to be an uncompetitive inhibitor. Structure-activity relationship studies indicated that the benzyloxy group present in compounds 12 and 13 is responsible for the beta-glucuronidase inhibition activity. |
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