Abstract
3,4-Dimethoxybenzohydrazide derivatives (1-25) have been synthesized and evaluated for their urease inhibitory potential. Among the series, compounds 2, 3, 4 and 5 with IC50 values 12.61 +/- 0.07, 18.24 +/- 0. 14, 19.22 +/- 0.21, and 8.40 +/- 0.05 mu M, respectively, showed excellent urease inhibitory potentials when compared with standard thiourea (IC50 value 21.40 +/- 0.21 mu M). Compounds 1, 6, 8, 18, 19 and 20 also showed good to moderate inhibition, while the remaining compounds were found to be completely inactive. The structures of compounds 6 and 25 were confirmed through X-ray crystallography while the structures of remaining compounds were confirmed through ESI-MS and H-1 NMR. Molecular docking studies were performed understand the binding interactions with enzyme active site. The synthesized compounds were evaluated for cytotoxicity and found to be nontoxic. (C) 2017 Elsevier Inc. All rights reserved.