期刊
DRUG DEVELOPMENT RESEARCH
卷 82, 期 4, 页码 533-542出版社
WILEY
DOI: 10.1002/ddr.21771
关键词
2‐ hydroxy‐ 4‐ methoxybenzamide; kinetic study; molecular docking; synthesis; tyrosinase inhibitor
资金
- Shiraz University of Medical Sciences
- [12626-106-01-95]
The novel 2-hydroxy-4-methoxybenzohydrazide showed promising tyrosinase inhibitory activity, with 4d being the most potent inhibitor. In vitro experiments and molecular modeling analysis suggested that 4d could be a potential candidate for developing anti-tyrosinase agents.
Due to the fact that tyrosinase is responsible for biosynthesis and regulation of melanins and browning food products, tyrosinase inhibitors can be favorable agents in cosmetics and medicinal industries. A series of novel 2-hydroxy-4-methoxybenzohydrazide were designed, synthesized, and their new application as tyrosinase inhibitors was also disclosed. Based on in vitro tyrosinase inhibitory assay, 4d as the strongest inhibitor of tyrosinase with an IC50 value of 7.57 mu M showed approximately 2.5-fold better inhibition than kojic acid as positive control followed by two compounds 4b (IC50 = 8.19 +/- 0.25 mu M) and 4j (IC50 = 8.92 +/- 0.016) which displayed preferable tyrosinase inhibitory activity. Detailed investigations on the mechanism of action of the 4d reported mix type of inhibition. More importantly, molecular modeling assessments proposed the ability of 4d for potential interaction with Cu (metal)-His (residue) within tyrosinase active site. Overall, 4d is a promising candidate for the development of anti-tyrosinase agents.
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