6757-36-4Relevant 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.
CCK-1 RECEPTOR MODULATORS
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Page/Page column 162, (2010/02/10)
There are provided by the present invention certain pyrazole based CCK-1 receptor modulators which have the general formula: (I) wherein Ar is an aromatic or heteroaromatic group, X is a hydrocarbon linker, Y is a bond or hydrocarbon linker and R1, R2, R3, R4 and R5 are certain organic substituents, and methods of making the same.
Reactions of cationic (η6-chloroarene) complexes of iron and ruthenium with some O-silyl and C-silyl compounds
Cambie, Richard C.,Coulson, Sally A.,Mackay, Lindsey G.,Janssen, Sally J.,Rutledge, Peter S.,Woodgate, Paul D.
, p. 385 - 409 (2007/10/02)
The introduction of an alylcarbonyl side chain into the aromatic ring of some chloro-substituted benzenes has been achieved under mild conditions by the Yanovsky-type reaction of (η6-chloroarene)(η5-cyclopentadienyl) cationic complex
