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The SAR analysis of TRPV1 agonists with the α-methylated B-region.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Aug 15; Vol. 22 (16), pp. 5227-31. Date of Electronic Publication: 2012 Jun 23. - Publication Year :
- 2012
-
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22796184
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.06.059