Synthesis of 2-substituted-pyrrolidinethiourea derivatives and their antagonist effect on vanilloid receptor

被引:14
作者
Park, HG [1 ]
Park, MK
Choi, JY
Choi, SH
Lee, J
Suh, YG
Oh, U
Lee, J
Kim, HD
Park, YH
Jeong, YS
Choi, JK
Jew, SS
机构
[1] Seoul Natl Univ, Pharmaceut Sci Res Inst, 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, Youngin Si 449900, Kyounggi Do, South Korea
关键词
D O I
10.1016/S0960-894X(02)00887-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Four pyrrolidine derivatives were prepared by the formation of a 5-membered ring based on capsazepine. Among them, the two carbon extended derivatives, 4a (IC50 = 55 muM) and 4b (IC50 = 3 muM), both showed different levels of antagonist activity against the vanilloid receptor in a Ca-45(2+)-influx assay. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:197 / 200
页数:4
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