129409-54-7Relevant articles and documents
2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists
Ann, Jihyae,Bahrenberg, Gregor,Blumberg, Peter M.,Choi, Sun,Christoph, Thomas,Do, Nayeon,Frank-Foltyn, Robert,Ha, Heejin,Jeong, Jin Ju,Kang, Jin Mi,Kim, Changhoon,Kwon, Sun Ok,Lee, Jeewoo,Lee, Sunho,Lesch, Bernhard,Stockhausen, Hannelore,Vu, Thi Ngoc Lan,Yoon, Sanghee
, (2021/07/28)
A series consisting of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists. The structure–activity analysis targeting their three pharmacophoric regions indicated that halogenated phenyl A-region analogs exhibited a broad functional profile ranging from agonism to antagonism. Among the compounds, antagonists 28 and 92 exhibited potent antagonism toward capsaicin for hTRPV1 with Ki[CAP] = 2.6 and 6.9 nM, respectively. Further, antagonist 92 displayed promising analgesic activity in vivo in both phases of the formalin mouse pain model. A molecular modeling study of 92 indicated that the two fluoro groups in the A-region made hydrophobic interactions with the receptor.
MULTIPLE KINASE PATHWAY INHIBITORS
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Page/Page column 267-269; 272, (2014/04/17)
Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
Process for the preparation of fluorophenylalkylene acid derivatives
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Page 12, (2010/02/09)
The invention relates to the preparation of fluorophenylalkylene acid derivatives of the formulae (4-1)-(4-3): by reaction between fluoroarylmetal halides of formulae (1-1) or (1-2) with carboxylic acid derivatives of formulae (2-1)-(2-3): in the presence