Methimazole의 Pro-drug들에 의한 Melanin생성 억제와 생물활성
Inhibition of Melanin Synthesis by Pro-drug of Methimazole and Their Bioactivity
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본 연구에서는 methimazole의 carbamate와 urea형의 pro-drug을 합성하여 그들의 melanin 합성억제 효과를 연구하였다. 대부분 carbamate 화합물들이 B16 cell에서 melanin 합성을 억제하였다, 그러나 mushroom tyrosinase를 직접 억제하지 않았고, 항산화 및 항당화작용을 보이지 않았다. 1번 화합물만 항산화작용을 중간정도로 보였다. 화합물 1과 20의 B16 cell 에서의 멜라닌 합성 억제는 약하였고 화합물 21과 27은 중간정도의 메라닌 합성 억제를 독성과 함께 보였다. 모든 urea형의 pro-drug들은 독성을 보였다. 화합물 20과 21을 중심으로 새로운 유도체와 그들의 활성실험이 진행중에 있다. 이들 methimazole의 pro-drug은 피부 미백제로서의 가능성을 보여줄 것이다.
Abstract
A small series of carbamate and urea pro-drugs of methimazole was synthesized and tested as melanin synthesis inhibitors. Most of carbamate compounds inhibited melanin synthesis in B16 cells, but many of them were inactive against mushroom tyrosinase activity, oxdation and glycation except for compound 1 which showed moderate activity of anti-oxidation. The activity of compounds 1 and 20 was weak in the inhibition of melanin synthesis in B16 cells, and compounds 21 and 27 showed moderate activity with toxicity. All of the urea prodrugs showed toxicity. The preparation of the other analogs derived from compounds 20 and 21 as well as their biological assays is ongoing. These prodrugs of methimazole may provide therapeutic potential as skinwhitening agents.
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