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Synthesis and Evaluation of 2(3H)-Thiazole Thiones as Tyrosinase Inhibitors
Emami, Saeed,Hosseinimehr, Seyed Jalal,Shahrbandi, Kami,Enayati, Ahmad Ali,Esmaeeli, Zahra
, p. 629 - 637 (2012/09/22)
A series of 2(3H)-thiazole thiones 3-5 was synthesized and evaluated for tyrosinase inhibition and DPPH radical scavenging activities. Among them, 3-methyl-4-phenyl-2(3H)-thiazole thione (4a) showed good tyrosinase inhibitory activity, even better than that of the well-known tyrosinase inhibitor, namely, kojic acid. From the structure-activity point of view, although it was found that the phenolic hydroxyl group in prototype 3-5 might contribute to the scavenging activity against DPPH radicals, there was no correlation between the potency of tyrosinase inhibition and the presence of the phenolic moiety. The in silico ADME-Tox screening revealed that the drug-likeness and drug-score values of the most potent compound 4a were significantly higher than those of kojic acid. Copyright
