@article{8fe80618aafc4371b0dc2b69f45d8351,
title = "N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region",
abstract = "Structure-activity relationships for the A-region in a series of N-4-t-butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamides as TRPV1 antagonists have been investigated. Among them, the 3-fluoro analogue 54 showed high binding affinity and potent antagonism for both rTRPV1 and hTRPV1 in CHO cells. Its stereospecific activity was demonstrated with marked selectivity for the (S)-configuration (54S versus 54R). A docking study of 54S with our hTRPV1 homology model highlighted crucial hydrogen bonds between the ligand and the receptor contributing to its potency.",
keywords = "Analgesic, Capsaicin, Molecular modeling, Resiniferatoxin, TRPV1 antagonists",
author = "Kim, {Yong Soo} and Kil, {Min Jung} and Kang, {Sang Uk} and Hyungchul Ryu and Kim, {Myeong Seop} and Yongsung Cho and Bhondwe, {Rahul S.} and Thorat, {Shivaji A.} and Wei Sun and Keliang Liu and Lee, {Jin Hee} and Sun Choi and Pearce, {Larry V.} and Pavlyukovets, {Vladimir A.} and Morgan, {Matthew A.} and Richard Tran and Jozsef Lazar and Blumberg, {Peter M.} and Jeewoo Lee",
note = "Funding Information: This research was supported by Research Funding from Digitalbiotech, Grants R11–2007–107–02001-0 from the National Research Foundation of Korea (NRF), the National Core Research Center (NCRC) program (No. 2011-0006244) of MEST and NRF through the Center for Cell Signaling & Drug Discovery Research at Ewha Womans University, and the intramural program of the National Institutes of Health, Center for Cancer Research, National Cancer Institute (project Z1A BC 005270).",
year = "2012",
month = jan,
day = "1",
doi = "10.1016/j.bmc.2011.11.008",
language = "English",
volume = "20",
pages = "215--224",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Ltd.",
number = "1",
}