Beta-N-cyanoethyl acyl hydrazide derivatives: a new class of beta-glucuronidase inhibitors.
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.
Khan
Khalid Mohammed
KM
H.E.J. Research Institute of Chemistry, International Centre for Chemical Sciences, University of Karachi, Pakistan. hasaan2@super.net.pk
Shujaat
Shahida
S
Rahat
Shagufta
S
Hayat
Safdar
S
Atta-ur-Rahman
Choudhary
Muhammad Iqbal
MI
D000818:Animals; D002417:Cattle; D005966:Glucuronidase / Q000037:antagonists & inhibitors*; D006023:Glycoproteins / Q000737:chemistry*; D006834:Hydrazines / Q000737:chemistry*
D006023:Glycoproteins; D006834:Hydrazines; C011473:beta-glucuronidase inhibitor; D005966:Glucuronidase