Continued SAR exploration of 1,2,4-thiadiazole-containing scaffolds in the design of free fatty acid receptor 1 (GPR40) agonists
Eur. J. Med. Chem. 2017, 140, 229–238
DOI: 10.1016/j.ejmech.2017.09.019
Krasavin M.; Lukin A.; Bakholdina A.; Zhurilo N.; Onopchenko O.; Borysko P.; Zozulya S.; Moore D.;
Tikhonova I. G.
Six sets of functionalized building blocks based on 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine as well as 5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-a]pyridine cores have been prepared. These compounds are non-flat, bicyclic heterocycles that are likely to find utility as privileged motifs for lead-like compound design. One set of building blocks, (5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-6-ylmethyl)amines, proved useful as a scaffold for developing compounds that stimulate glucagon-like peptide-1 (GLP-1) secretion and are novel anti-diabetes drug leads.
