2. Academic Validation
  3. The SAR analysis of TRPV1 agonists with the α-methylated B-region

The SAR analysis of TRPV1 agonists with the α-methylated B-region

  • Bioorg Med Chem Lett. 2012 Aug 15;22(16):5227-31. doi: 10.1016/j.bmcl.2012.06.059.
Yongsung Cho 1,  Myeong Seop Kim,  Ho Shin Kim,  Jihyae Ann,  Jiyoun Lee,  Larry V Pearce,  Vladimir A Pavlyukovets,  Matthew A Morgan,  Peter M Blumberg,  Jeewoo Lee
Affiliations

Affiliation

  • 1 Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
PMID: 22796184 DOI: 10.1016/j.bmcl.2012.06.059
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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