15917-88-1Relevant academic research and scientific papers
Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Li, Zheng,Wang, Xuekun,Xu, Xue,Yang, Jianyong,Xia, Wenting,Zhou, Xianhao,Huang, Wenlong,Qian, Hai
supporting information, p. 7158 - 7164 (2015/11/16)
The free fatty acid receptor 1 (FFA1) is a novel antidiabetic target for the treatment of type 2 diabetes based on particular mechanism in amplifying glucose-stimulated insulin secretion. We have previously identified a series of phenoxyacetic acid deriva
2-Thiohydantoine derivative compounds and use thereof for the treatment of diabetes
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Page/Page column 10, (2010/02/15)
The invention relates to 2-thiohydantoin compounds selected from compounds of general formula (I): in which, in particular, one of the radicals R1 and R2 comprises two aromatic rings in the structure or is the dibenzofuranyl group, R3 is a hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxy group, a hydroxyl group, a phenyl group or a benzyl group, R4 is a hydrogen atom, a halogen atom or a C1-C4 alkyl group, and their addition salts with a non-toxic acid, especially the pharmaceutically acceptable salts. It further relates to the process for their preparation, to the pharmaceutical compositions in which they are present, and to their use as pharmacologically active substances, especially in the case of the treatment of diabetes, diseases due to hyperglycemia, hypertriglyceridemia, dyslipidemia or obesity.
Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives
Stanton,Gruenfeld,Babiarz,Ackerman,Friedmann,Yuan,Macchia
, p. 1267 - 1277 (2007/10/02)
The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x), -N-arylalanines (15a,b), -N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure-activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 x 10-9 M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.
