Original articleSynthesis and biological evaluation of novel 4-Hydroxybenzaldehyde (cas 123-08-0) derivatives as tyrosinase inhibitors
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Add time:09/08/2019 Source:sciencedirect.com
A series of novel 4-Hydroxybenzaldehyde (cas 123-08-0) derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were investigated. Most of target compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). Interestingly, compound 3c bearing a dimethoxyl phosphate was found to be the most potent inhibitor with IC50 value of 0.059 mM. The inhibition kinetics analyzed by Lineweaver–Burk plots revealed that compound 3c was a non-competitive inhibitor (KI = 0.0368 mM). In particular, compound 3c showed no side effects at dose of 1600 mg/kg in mice. These results suggested that such compounds might be served as lead compounds for further designing new potential tyrosinase inhibitors.
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