Design, synthesis and biological evaluation of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones as tyrosinase inhibitors. Chemical & pharmaceutical bulletin [Chem Pharm Bull (Tokyo)] Journal article | | Title | Design, synthesis and biological evaluation of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones as tyrosinase inhibitors. | | Author(s) | Yi W, Cao RH, Chen ZY, Yu L, Ma L, Song HC | | Institution | School of Chemistry and Chemical Engineering, Sun Yat-sen University. | | Source | Chem Pharm Bull (Tokyo) 2009 Nov; 57(11):1273-7. | | Abstract | A series of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones were designed, synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of target compounds had remarkable inhibitory activities on mushroom tyrosinase. Interestingly, compound 2h was found to be the most potent tyrosinase inhibitor with IC(50) value of 0.18 muM. The possible interaction mode between compound 2h and tyrosinase was proposed. In addition, the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities of select compounds (IC(50)<10.0 muM) were also investigated. Compounds 2d, 2e, 2h, 2i and 2l exhibited more potent DPPH radical scavenging activity than well-known antioxidants ascorbic acid (Vc) and tertiary butyl hydroquinone (TBHQ). These results suggested that such compounds might be utilized for the development of new candidate for treatment of dermatological disorders. | | Language | eng | | Pub Type(s) | Journal Article
| | PubMed ID | 19881280 |
|
|
| |
Advertise on this site.
| | |
|
