172168-01-3Relevant articles and documents
Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists
Shu, Shuangjie,Cai, Xiaoqing,Li, Jia,Feng, Yang,Dai, Antao,Wang, Jiang,Yang, Dehua,Wang, Ming-Wei,Liu, Hong
, p. 2852 - 2863 (2016/06/08)
Glucagon receptor antagonists possess a great potential for treatment of type 2 diabetes mellitus. A series of pyrazole-containing derivatives were designed, synthesized and evaluated by biological assays as glucagon receptor antagonists. Most of the compounds exhibited good in vitro efficacy. Two of them, compounds 17f and 17k, displayed relatively potent antagonist effects on glucagon receptors with IC50 values of 3.9 and 3.6 μM, respectively. The possible binding modes of 17f and 17k with the cognate receptor were explored by molecular docking simulation.
Synthesis and pharmacological evaluation of a new series of substituted benzoyl-γ-butyrolactone derivatives
Cignarella, G.,Barlocco, D.,Pocar, D.,Clerici, F.,Curzu, M. M.,et al.
, p. 721 - 726 (2007/10/03)
A series of substituted benzoyl-γ-butyrolactones (1-3) has been synthesized and tested for their ability to affect central dopaminergic and GABAergic function in comparison to γ-butyrolactone (GBL).Similarly to GBL, α-, β- and γ-substituted GBLs 1-3 with one or more chlorine on the phenyl ring were found to induce central depressant effects in rats, though at different degrees.However, the test compounds modified dopamine (DA) metabolism in rat striatum differently from GBL.In fact, whereas GBL increased both DA and dihydroxyphenylacetic acid (DOPAC) content, GBL derivatives 1-3 increased DA levels, but reduced the DOPAC concentration.Moreover, some of them, unlike GBL, effectively antagonized pentylenetetrazole (PTZ)-induced seizures in mice.In particular, α-3,5-dichlorobenzoyl-GBL (1g) was effective at a dose as low a 36 mg/kg in decressing the number of animals having convulsions.However, in vitro addition and in vivo administration of the test compounds failed to modify -t-butylbicyclophosphorothionate (-TBPS) binding, which is a very sensitive tool for revealing changes in the GABAergic function. γ-butyrolactone / benzoyl-γ-butyrolactone / dopamine / anticonvulsant effect
