- Rational design and synthesis of 4-O-substituted phenylmethylenethiosemicarbazones as novel tyrosinase inhibitors
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In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have significant tyrosinase inhibitiory activity. Particularly, the IC50 values of compounds 3a-g, 3j and 3s were of the same magnitude as tropolone, one of the best tyrosinase inhibitors known so far. Furthermore, the structure-activity relationships of these compounds were also investigated. All these data suggested that these molecules might be utilized for the development of new candidate for the treatment of dermatological disorders, and further development of such compounds may be of interest.
- Yi, Wei,Cao, Rihui,Chen, Zhiyong,Yu, Liang,Wen, Huan,Yan, Qin,Ma, Lin,Song, Huacan
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experimental part
p. 752 - 754
(2010/07/15)
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- Synthesis and properties of Schiff's bases derived from 1,3,4-thiadiazole as a mesogenic unit
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Some new liquid crystalline 2,5-disubstituted 1,3,4-thiadiazole derivatives incorporating a central group (-CH=N-) have been synthesized by treating 2-amino-5-(4-alkoxyphenyl)-1,3,4-thiadiazole with corresponding p-alkoxybenzaldehyde. Their structures have been characterized with Elementary Analysis, IR, 1HNMR and MS, and their properties were determined by using DSC and Texture. All 12 compounds are enantiotropic liquid crystals, and most of them exhibit nematic mesomorphism and broad smectic C mesomorphic ranges. Several compounds show only the smectic C mesophase. By introducing an -OH group into the phenyl ring the thermal stability of the mesophases increases due to the formation of a hydrogen bond.
- Xu,Lu,Tai
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p. 151 - 159
(2007/10/03)
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