Synthesis and in聽vitro urease inhibitory activity of N,N鈥?/span>-disubstituted thioureas

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• 作者：Khalid Mohammed Khan^a ; ^{hassaan2@super.net.pk" class="auth_mail} ; ^{khalid.khan@iccs.edu" class="auth_mail} ; Farzana Naz^a ; Muhammad Taha^b ; ^d ; Ajmal Khan^a ; Shahnaz Perveen^c ; M.I. Choudhary^a ; Wolfgang Voelter^e
• 关键词：Thiourea derivatives ; Synthesis ; In vitro urease inhibition activity ; Kinetic study
• 刊名：European Journal of Medicinal Chemistry
• 出版年：3 March, 2014
• 年：2014
• 卷：74
• 期：Complete
• 页码：314-323
• 全文大小：1448 K

文摘

Thiourea derivatives (1-38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in聽vitro urease inhibition with IC₅₀ values 5.53聽卤聽0.02-91.50聽卤聽0.08聽渭M, most of which are superior to the standard thiourea (IC₅₀聽=聽21.00聽卤聽0.11聽渭M). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29聽渭M.