化学
酪氨酸酶
哌嗪
肉桂酸
酰胺
对接(动物)
生物信息学
铅化合物
IC50型
组合化学
立体化学
生物化学
酶
有机化学
体外
基因
护理部
医学
作者
Zehra Tuğçe Gür,Fatma Sezer Şenol,Suhaib Shekfeh,İlkay Erdoğan Orhan,Erden Banoğlu,Burcu Çalışkan
标识
DOI:10.2174/1570180815666180420105652
摘要
Background: A series of novel cinnamic acid piperazine amide derivatives has been designed and synthesized, and their biological activities were also evaluated as potential tyrosinase inhibitors. Methods: Compounds 9, 11 and 17 showed the most potent biological activity (IC50 = 66.5, 61.1 and 66 µM, respectively). In silico docking simulation was performed to position compound 11 into the Agaricus bisporus mushroom tyrosinase’s active site to determine the putative binding interactions. Results and Conclusion: The results indicated that compound 11 could serve as a promising lead compound for further development of potent tyrosinase inhibitors.
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