| Literature DB >> 22227463 |
Wei Sun1, Keliang Liu, HyungChul Ryu, Dong Wook Kang, Yong Soo Kim, Myeong Seop Kim, Yongsung Cho, Rahul S Bhondwe, Shivaji A Thorat, Ho Shin Kim, Larry V Pearce, Vladimir A Pavlyukovets, Richard Tran, Matthew A Morgan, Jozsef Lazar, Christopher B Ryder, Attila Toth, Peter M Blumberg, Jeewoo Lee.
Abstract
On the basis of the previous lead N-4-t-butylbenzyl 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamide (3) as a potent TRPV1 antagonist, structure-activity relationships for the B (propanamide part) and C-region (4-t-butylbenzyl part) have been investigated for rTRPV1 in CHO cells. The B-region was modified with dimethyl, cyclopropyl and reverse amides and then the C-region was replaced with 4-substituted phenyl, aryl alkyl and diaryl alkyl derivatives. Among them, compound 50 showed high binding affinity with K(i)=21.5nM, which was twofold more potent than 3 and compound 54 exhibited potent antagonism with K(i(ant))=8.0nM comparable to 3.Entities:
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Year: 2011 PMID： 22227463 PMCID： PMC6988731 DOI： 10.1016/j.bmc.2011.12.014
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641