Synthesis of N, N′, N ″-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor

H Park, M Park, J Choi, S Choi, J Lee, B Park…

Index: Park, Hyeung-Geun; Park, Mi-Kyung; Choi, Ji-Yeon; Choi, Sea-Hoon; Lee, Jihye; Park, Boon-Saeng; Kim, Myoung Goo; Suh, Young-Ger; Cho, Hawon; Oh, Uhtaek; Lee, Jeewoo; Kim, Hee-Doo; Park, Young-Ho; Koh, Hyun-Ju; Lim, Kyung Min; Moh, Joo-Hyun; Jew, Sang-Sup Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 4 p. 601 - 604

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Citation Number: 24

Abstract

Twenty-seven N, N′, N ″-trisubstituted thiourea derivatives were prepared. Among them, 1- [3-(4′-hydroxy-3′-methoxy-phenyl)-propyl]-1, 3-diphenethyl-thiourea (8l, IC50= 0.32 μM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC50= 0.65 μM) against the vanilloid receptor in a 45Ca2+-influx assay.