Synthesis and urease inhibitory activities of benzophenone semicarbazones/thiosemicarbazones
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- 作者：Arshia Arshia ; Ajmal Khan ; Khalid Mohammed Khan…
- 关键词：Benzophenone ; Semicarbazone ; Thiosemicarbazone ; Ureases inhibition ; Structure ; activity relationship
- 刊名：Medicinal Chemistry Research
- 出版年：2016
- 出版时间：November 2016
- 年：2016
- 卷：25
- 期：11
- 页码：2666-2679
- 全文大小：883 KB
- 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
- 出版者：Springer US
- ISSN：1554-8120
- 卷排序：25
文摘
Twenty-five benzophenone semicarbazones and thiosemicarbazones 3–27 were synthesized starting from benzophenones via hydrazones treated with different aryl isocyanates and isothiocyantes under reflux. All synthetic derivatives were evaluated for their urease inhibitory potential. Good to moderate inhibition trend against urease was observed with the IC50 values in the range of 8.7–119.5 µM, when compared with the standard thiourea (IC50 = 21.2 ± 1.3 µM). Compound 15 showed better inhibition than the standard having the IC50 value of 8.7 ± 0.6 µM. Compounds 3, 4, 8, 11–14, 16, and 17 with the IC50 values within the range of 26.1 to 43.6 µM, demonstrated good to moderate activities while compound 9 (IC50 = 119.5 ± 1.6 µM) displayed very weak activity. The enzyme kinetic studies on the most active compounds 15 and 17 were performed to deduce their modes of inhibition and dissociation constants Ki.