title: Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists.
abstract: We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent (45)Ca(2+) uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC(50) of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described.
authors.affiliation: College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors.forename: Fu-Nan
authors.initials: FN
authors.lastname: Li
authors.forename: Nam-Jung
authors.initials: NJ
authors.lastname: Kim
authors.forename: Seung-Mann
authors.initials: SM
authors.lastname: Paek
authors.forename: Do-Yeon
authors.initials: DY
authors.lastname: Kwon
authors.forename: Kyung Hoon
authors.initials: KH
authors.lastname: Min
authors.forename: Yeon-Su
authors.initials: YS
authors.lastname: Jeong
authors.forename: Sun-Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Hee-Doo
authors.initials: HD
authors.lastname: Kim
authors.forename: Hyeung-Geun
authors.initials: HG
authors.lastname: Park
authors.forename: Young-Ger
authors.initials: YG
authors.lastname: Suh
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002478:Cells, Cultured; D015195:Drug Design; D020128:Inhibitory Concentration 50; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000577:Amides; C541658:N-(3-cyano-5-fluoro-4-(methylsulfonamido)benzyl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)propanamide; D013449:Sulfonamides; D050916:TRPV Cation Channels; D013764:Tetrahydronaphthalenes; C493922:Trpv1 protein, rat; D002118:Calcium