1372195-41-9

Upstream product

• 691905-27-8 (2',6'-dimethyl-[1,1'-biphenyl]-3-yl)methanol 
• 123-08-0 4-hydroxy-benzaldehyde 
• 588676-02-2 4-((3-bromobenzyl)oxy)benzaldehyde 
• 100379-00-8 2,6-dimethylbenzene boronic acid 
• 15852-73-0 (3-Bromophenyl)methanol 

Downstream Products

• 1372195-46-4 2-(4-((2',6'-dimethyl-[1,1'-biphenyl]-3-yl)methoxy)phenyl)-N,N-bis(4-methoxybenzyl)ethenesulfonamide 
• 1372195-43-1 ethyl 3-amino-3-(4-((2',6'-dimethyl-[1,1'-biphenyl]-3-yl)methoxy)phenyl)propionate 
• 1372195-48-6 dimethyl 2-(2-(N,N-bis(4-methoxybenzyl)sulfamoyl)-1-(4-((2',6'-dimethyl-[1,1'-biphenyl]-3-yl)methoxy)phenyl)ethyl)malonate 
• 1372195-51-1 methyl 3-(4-((2',6'-dimethyl-[1,1'-biphenyl]-3-yl)methoxy)phenyl)-4-sulfamoylbutanoate 
• 1372195-49-7 methyl 4-(N,N-bis(4-methoxybenzyl)sulfamoyl)-3-(4-((2',6'-dimethyl-[1,1'-biphenyl]-3-yl)methoxy)phenyl)butanoate 
• 1372192-11-4 5-[4-[[3-(2,6-dimethylphenyl)phenyl]methoxy]phenyl]-1,1-dioxo-1,2-thiazinan-3-on 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of novel thiazolidinediones as PPAR3/FFAR1 dual agonists

Diabetes mellitus is a chronic metabolic disorder that affects more than 180 million people worldwide. Peroxisome proliferator activated receptors (PPARs) are a group of nuclear receptors that have been targeted by the thiazolidinedione (TZD) class of compounds for the management of type II diabetes. PPAR3 is known to regulate adipogenesis and glucose metabolism. Another emerging target for the design of antidiabetic agents is the free fatty acid receptor 1 (FFAR1), previously known as GPR40. Agonists of this receptor were found to enhance insulin secretion in diabetic patients. It has been reported that some thiazolidinediones (TZDs) activate FFAR1 with micromolar potency. In this study, based on docking studies into the crystal structure of PPAR3 and a homology model of FFAR1, nineteen compounds were designed, synthesized, and biologically tested for agonistic activity on both receptors. Nine compounds showed promising dual activity, with two compounds, 11a and 5b, having affinities in the low micromolar range on both targets. These molecules represent the first antidiabetic agents that could act as insulin sensitizers as well as insulin secretagogues.

CYCLIC AMIDE DERIVATIVE

[Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.