作者
Aamer Saeed, Sajid-ur Rehman, Pervaiz Ali Channar, Fayaz Ali Larik, Qamar Abbas, Mubashir Hassan, Hussain Raza, Ulrich Flörke, Sung-Yum Seo
发表日期
2017/8/1
期刊
Journal of the Taiwan Institute of Chemical Engineers
卷号
77
页码范围
54-63
出版商
Elsevier
简介
The current research work reports the synthesis of novel long chain acyl thiourea derivatives as inhibitors of jack bean ureas. The title compounds were synthesized by the conversion of long chain carboxylic acids into corresponding acid chlorides followed by reaction with potassium thiocyanate to obtain a key reactive intermediate isothiocyanate, the latter was treated with suitably substituted aromatic anilines to afford the title 1-(substituted)phenyl-3-tetradecanoylthioureas. All of the compounds showed higher urease inhibitory activity than the standard thiourea. The compound 5f exhibited excellent enzyme inhibitory activity with IC50 0.0391 ± 0.0028 µM while IC50 of thiourea is 18.195 ± 0.382 µM. The kinetic mechanism analyzed by Lineweaver–Burk plots showed that compound 5f is a non-competitive type inhibitor. Docking studies suggested that Asp494, Ala636, His593, Ala636, Lue494, Asp521 and …
学术搜索中的文章
A Saeed, S Rehman, PA Channar, FA Larik, Q Abbas… - Journal of the Taiwan Institute of Chemical Engineers, 2017