The series of imidazoldine-2-thiones 2 and tetrahydropyrimidine-2-thiones 3 were discovered as inhibitor of α-MSH-induced melanin production in melanoma B16 cells. The primary bioassay showed that 1-(4-ethylbenzyl)-tetrahydropyrimidine-2 (1H)-thione 3e (> 100% inhibition at 10μM, IC50= 1.2 μM) and 1-(4-tert-butylbenzyl)-tetrahydropyrimidine-2 (1H)-thione 3f (> 100% inhibition at 10μM, IC50= 0.76 μM) exhibited potent inhibitory ...