Novel Piperazine Amides of Cinnamic Acid Derivatives as Tyrosinase Inhibitors

Author(s): Zehra Tuğçe Gür, Fatma Sezer Şenol, Suhaib Shekfeh, İlkay Erdoğan Orhan, Erden Banoğlu, Burcu Çalişkan*.

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 1 , 2019

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Graphical Abstract:


Abstract:

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.

Keywords: Ferulic acid, cinnamic acid, piperazine, tyrosinase, docking, huntington's diseases.

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Article Details

VOLUME: 16
ISSUE: 1
Year: 2019
Page: [36 - 44]
Pages: 9
DOI: 10.2174/1570180815666180420105652
Price: $58

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