1300747-67-4

Basic information

• Product Name: 5-(4-nitrophenyl)thiazole-2-carboxylic acid
• Synonyms: 5-(4-nitrophenyl)thiazole-2-carboxylic acid
• CAS NO: 1300747-67-4
• Molecular Weight: 250.235
• Mol File: 1300747-67-4.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 5-(4-nitrophenyl)thiazole-2-carboxylic acid(CAS DataBase Reference)
• NIST Chemistry Reference: 5-(4-nitrophenyl)thiazole-2-carboxylic acid(1300747-67-4)
• EPA Substance Registry System: 5-(4-nitrophenyl)thiazole-2-carboxylic acid(1300747-67-4)

Safety Data

• Hazardous Substances Data: 1300747-67-4(Hazardous Substances Data)

Upstream product

• 4740-22-1 2-amino-1-(4-nitro-phenyl)-ethanone 
• 1300747-66-3 ethyl 5-(4-nitrophenyl)thiazole-2-carboxylate 
• 2082-12-4 ethyl 2-((2-(4-nitrophenyl)-2-oxoethyl)amino)-2-oxoacetate 
• 100-19-6 (4-nitrophenyl)ethanone 
• 99-81-0 4-Nitrophenacyl bromide 
• 5425-81-0 2-amino-1-(4-nitrophenyl)ethanone hydrochloride 

Relevant articles and documents

Synthesis and evaluation of cyclohexane carboxylic acid head group containing isoxazole and thiazole analogs as DGAT1 inhibitors

Diacylglycerol acyltransferase 1 (DGAT1) is known to play an important catalytic role in the final step of triglyceride biosynthesis. High fat diet fed DGAT1 knockout mice were resistant to weight gain and exhibited increased insulin and leptin sensitivity thereby indicating a plausible role for DGAT1 inhibitors in the treatment of obesity. 4-Phenylpiperidine-1-carbonyl cyclohexanecarboxylic acid (compound 6, DGAT1 IC50 = 57 nM) has been lately reported as a potent DGAT1 inhibitor. In our search for newer scaffolds possessing potent DGAT1 activity we undertook a systematic diversification of compound 6 to identify a 4-(5-phenylthiazole-2-carboxamido)cyclohexanecarboxylic acid scaffold. Further linker optimization of this scaffold identified compound 9e (DGAT1 IC50 = 14.8 nM) as a potent DGAT1 inhibitor. Coupled with its in vitro potency, compound 9e also exhibited 112 percent plasma triglyceride reduction at a 3 mpk dose in an oral fat tolerance test (FTT) when studied in Swiss mice.

HETEROARYL COMPOUNDS AS DGAT-1 1NHIBITORS

The present invention relates to novel heteroaryl compounds, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or disorders mediated by Diacylglycerol acyltransferase (DGAT) enzyme, particularly DGAT- 1.