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

被引:21
作者
Park, H [1 ]
Park, M
Choi, J
Choi, S
Lee, J
Park, B
Kim, MG
Suh, Y
Cho, H
Oh, U
Lee, J
Kim, HD
Park, YH
Koh, HJ
Lim, KM
Moh, JH
Jew, S
机构
[1] Seoul Natl Univ, Res Inst Pharmaceut Sci, Seoul 151742, South Korea
[2] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea
[3] Sookmyung Womens Univ, Coll Pharm, Seoul 140742, South Korea
[4] AmorePacific R&D Ctr, Kyounggi 449900, South Korea
关键词
D O I
10.1016/S0960-894X(02)01040-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Twenty-seven N,N',N"-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4'-hydroxy-3'-methoxy- phenyl)-propyl]-1.3-diphenethyl-thiourea (81, IC50=0.32 muM), showed 2-fold higher antagonistic actively than that of capsazepine (3, IC50 = 0.65 muM) against the,anilloid receptor in a Ca-45(2+)-influx assay. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:601 / 604
页数:4
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