| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371253 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogues were investigated. Whereas the α-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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,