Sato, Kenjiro published the artcileDiscovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists, COA of Formula: C8H8ClN, the main research area is indoline carbamate indolinylpyrimidine preparation GPR119 agonist; Conformation; GPCR; GPR119 agonist; Indoline; Type 2 diabetes mellitus.
GPR119 has emerged as an attractive target for antidiabetic agents. The authors identified a structurally novel GPR119 agonist that carries a 5-(methylsulfonyl)indoline motif as an early lead compound To generate more potent compounds of this series, structural modifications were performed mainly to the central alkylene spacer. Installation of a carbonyl group and a Me group on this spacer significantly enhanced agonistic activity, resulting in the identification of I. To further expand the chem. series of indoline-based GPR119 agonists, several heterocyclic core systems were introduced as surrogates of the carbamate spacer that mimic the presumed active conformation. This approach successfully produced an indolinylpyrimidine II, which has potent GPR119 agonist activity. In rat oral glucose tolerance tests, these two indoline-based compounds effectively lowered plasma glucose excursion and glucose-dependent insulin secretion after oral administration.
Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, COA of Formula: C8H8ClN.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles