112596-36-8Relevant articles and documents
Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes
Li, Zheng,Pan, Miaobo,Su, Xin,Dai, Yuxuan,Fu, Mian,Cai, Xingguang,Shi, Wei,Huang, Wenlong,Qian, Hai
, p. 1981 - 1987 (2016)
The free fatty acid receptor 1 (FFA1) has gained significant interest as a novel antidiabetic target. Most of FFA1 agonists reported in the literature bearing a common biphenyl scaffold, which was crucial for toxicity verified by the researchers of Daiichi Sankyo. Herein, we describe the systematic exploration of non-biphenyl scaffold and further chemical modification of the optimal pyrrole scaffold. All of these efforts led to the identification of compound 11 as a potent and orally bioavailable FFA1 agonist without the risk of hypoglycemia. Further molecular modeling studies promoted the understanding of ligand-binding pocket and might help to design more promising FFA1 agonists.
Inhibition of Copper-Dependent Amine Oxidases by Some Hydrazides of Pyrrol-1-ylbenzoic and Pyrrol-1-ylphenylacetic Acids
Artico, Marino,Corelli, Federico,Massa, Silvio,Stefancich, Giorgio,Avigliano, Luciana,et al.
, p. 802 - 806 (2007/10/02)
Some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids were prepared, and their effect on copper-dependent amine oxidases (Cu-AOs) and FAD monoamine oxidases (MAOs) activities was tested.The compounds were not substrates for Cu-AO enzymes
