72278-52-5Relevant academic research and scientific papers
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
, p. 132 - 140 (2015/02/18)
Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
GHRH analogs
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, (2008/06/13)
There is provided a novel series of synthetic GHRH analog peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which are resistant to enzymatic degradation in the body in view of the provision of the omega-guanidino lower alkyl group at the terminal 28-position of the peptide.
Synthetic GHRH analogs
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, (2008/06/13)
Human pancreatic GRF (hpGRF), rat hypothalamic GRF (rGRF) and porcine hypothalamic GRF (pGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: STR1 wherein Q1 is an omega or alpha-omega substituted alkyl, Q2 is a lower omega-quanidino-alkyl group. R2 is Ala, D-Ala, or D-N-Methyl-Ala R3 is Asp, D-Asp, Glu, or D-Glu R8 is Asn, D-Asn, Ser, or D-Ser R10 is Tyr or D-Tyr R12 is Lys, D-Lys Arg or Orn R13 is Val or Ile R14 is Leu or D-Leu R15 is Gly, N-Methyl-Gly, or D-Ala R17 is Leu or D-Leu R18 is Tyr or Ser R23 is Leu or D-Leu R24 is Gln or His R25 is Asp, D-Asp, Glu, or D-Glu R27 is Met, D-Met, Ala, Nle, Ile, Val, Nva, Leu R28 is Asn or Ser The peptides as well as nontoxic salts thereof may be administered to animals, including humans and cold-blooded animals, to stimulate the release of GH and may be used diagnostically.
2,5,6,7-tetranor-4,8-inter-m-phenylene PGI2 derivatives
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, (2008/06/13)
Disclosed herein are novel prostaglandin I2 (PGI2) derivatives exhibiting excellent in vivo duration and activities, said derivatives being represented by the general formula: STR1 wherein R1, X, R2 and R3 are as defined herein.
