Inhibitory effect of novel tetrahydropyrimidine-2(1H)-thiones on melanogenesis

P. Thanigaimalai, Ki Cheul Lee, Seong Cheol Bang, Jee Hyun Lee, Cheong Yong Yun, Eunmiri Roh, Bang Yeon Hwang, Youngsoo Kim, Sang Hun Jung

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32 Scopus citations


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 10 μM, IC50 = 1.2 μM) and 1-(4-tert-butylbenzyl)-tetrahydropyrimidine-2(1H)-thione 3f (>100% inhibition at 10 μM, IC50 = 0.76 μM) exhibited potent inhibitory effect against α-MSH-induced melanin production. Compounds 3 inhibit the biosynthesis of tyrosinase without affecting its catalytic activity in melanogenesis.

Original languageEnglish (US)
Pages (from-to)1135-1142
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number3
StatePublished - Feb 1 2010

Bibliographical note

Funding Information:
This research was financially supported by a grant ( R01-2007-000-20099-0 ) from the National Research Foundation of Korea .


  • Hypopimenting
  • Melanogenesis
  • Tetrahydropyrimidine-2(1H)-thione
  • α-MSH-induced melanin production


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