The SAR analysis of TRPV1 agonists with the ¦Á-methylated B-region
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- 作者：Yongsung Cho ; Myeong Seop Kim ; Ho Shin Kim ; Jihyae Ann ; Jiyoun Lee ; Larry V. Pearce ; Vladimir A. Pavlyukovets ; Matthew A. Morgan ; Peter M. Blumberg ; Jeewoo Lee
- 关键词：Vanilloid receptor 1 ; TRPV1 agonist ; Capsaicin
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：15 August, 2012
- 年：2012
- 卷：22
- 期：16
- 页码：5227-5231
- 全文大小：902 K
文摘
A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding ¦Á-methylated analogues were investigated. Whereas the ¦Á-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The analysis indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.