Lee Jee-Hyun, Thanigaimalai Pillaiyar, Lee Ki-Cheul, Bang Seong-Cheol, Kim Min-Seok, Sharma Vinay Kumar, Yun Cheong-Yong, Roh Eunmiri, Kim Youngsoo, Jung Sang-Hun
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon, Korea.
Chem Pharm Bull (Tokyo). 2010 Jul;58(7):918-21. doi: 10.1248/cpb.58.918.
In order to determine the optimum size of heterocycle of lead compound 1 (6-methyl-3-phenethyl-3,4-dihydro-1H-quinoline-2-thione; IC(50)=0.8 microM) for inhibition of melanogenesis, we have synthesized and evaluated some benzimdazole-2(3H)-thiones 5a-e. The preliminary bioassay has shown that the benzimdazole-2(3H)-thione motif of 5 is essential structural unit for their inhibitory activity. Among all thiones 5a-e, the compound 5d strongly inhibited the formation of melanin with IC(50) value of 1.3 microM.
为了确定铅化合物1（6-甲基-3-苯乙基-3,4-二氢-1H-喹啉-2-硫酮；IC(50)=0.8微摩尔）抑制黑色素生成的杂环最佳尺寸，我们合成并评估了一些苯并咪唑-2(3H)-硫酮5a-e。初步生物测定表明，5的苯并咪唑-2(3H)-硫酮基序是其抑制活性的关键结构单元。在所有硫酮5a-e中，化合物5d强烈抑制黑色素形成，IC(50)值为1.3微摩尔。
