Design, synthesis, and urease inhibition studies of a series of 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones

A series of 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones was synthesized by reaction of aryl hydrazides with CS(2) and hydrazine hydrate. The synthesized compounds were characterized by spectroanalytical techniques, and their urease inhibition activity was evaluated using jack bean urease. All but one of the synthesized compounds were active, and two of them were found to be more potent than the standard, with 50% inhibition concentration (IC(50)) values of 17.5 +/- 0.52 and 4.3 +/- 0.169 mu M, respectively (standard IC(50) = 21.0 +/- 0.11 mu M). Tentative statements regarding the role of different functional groups in binding to the enzyme active site are also presented.