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Based on structure of the substrate of urease and for the purpose of designing pharmacophore models for urease inhibitors, which could be effective in physiological and pharmacological studies, a series of twenty-five 1,3,4-oxa diazole-2(3H)-thiones-2(3H)-thiones, 1,3,4-thia diazoles-2(3H)-thiones, and 1,2,4-triazole -3-thiones (OSNs) were designed, synthesized, and evaluated for various kinetic parameters of urease inhibition. OSNs inhibited the activity of urease(s) in a concentration dependent fashion. Dixon as well as Lineweaver–Burk plots and their secondary replots indicated that the nature of inhibition was of pure competitive type for all the 25 compounds. 5-[4-(hydroxy)phenyl]-1,3,4-thiadiazole-2(3H)-thione was found to be the most active one with a K_i value of 2μM. The K_i values were increased with an increase in substrate concentrations. Apparently, OSNs employ a homologous mechanism of action …