925439-32-3Relevant academic research and scientific papers
Discovery of a novel selective PPARγ modulator from (-)-Cercosporamide derivatives
Furukawa, Akihiro,Arita, Tsuyoshi,Satoh, Susumu,Wakabayashi, Kenji,Hayashi, Shinko,Matsui, Yumi,Araki, Kazushi,Kuroha, Masanori,Ohsumi, Jun
scheme or table, p. 2095 - 2098 (2010/08/22)
In an investigation of (-)-Cercosporamide derivatives with a plasma glucose-lowering effect, we found that N-benzylcarboxamide derivative 4 was a partial agonist of PPARγ. A SAR study of the substituents on carboxamide nitrogen afforded the N-(1-naphthyl)methylcarboxamide derivative 23 as the most potent selective PPARγ modulator. An X-ray crystallography study revealed that compound 23 bounded to the PPARγ ligand binding domain in a unique way without any interaction with helix12. Compound 23 displayed a potent plasma glucose-lowering effect in db/db mice without the undesirable increase in body fluid and heart weight that is typically observed when PPARγ full agonists are administrated.
NOVEL CERCOSPORAMIDE DERIVATIVE
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Page/Page column 83, (2008/06/13)
The present invention relates to a novel cercosporamide derivative, a pharmacologically acceptable salt thereof or an ester thereof which has an excellent hypoglycemic effect and is useful as a therapeutic and/or prophylactic agent for diabetes. A cercosporamide derivative having the general formula (I): [wherein X represents an oxygen atom or the like, R1 represents a hydrogen atom or a C1-C6 alkyl group, R2 represents a hydrogen atom, a C1-C6 alkyl group or a C1-C6 halogenated alkyl group, R3 represents a hydrogen atom or a C1-C6 alkyl group, R4 represents a C6-C10 aryl group which may be substituted with one to five group(s) independently selected from Substituent Group a, or the like, n represents 1, 2 or 3, and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, a C2-C6 alkenyloxy group, a C2-C6 alkynyloxy group and the like], a pharmacologically acceptable salt thereof or an ester thereof.
