In 2014,Kandre, Shivaji; Bhagat, Pundlik Rambhau; Kumar Reddy, M. Mahesh; Dalal, Roda; Dixit, Amol; Deshmukh, Nitin J.; Anthony, Jessy; Bose, Julie; Anupindi, Raghuram; Sharma, Rajiv; Gupte, Amol published 《Synthesis and evaluation of cyclohexane carboxylic acid head group containing isoxazole and thiazole analogs as DGAT1 inhibitors》.European Journal of Medicinal Chemistry published the findings.Related Products of 16982-21-1 The information in the text is summarized as follows:
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 has been lately reported as a potent DGAT1 inhibitor (DGAT1 IC50 = 57 nM). In the search for newer scaffolds possessing potent DGAT1 activity the authors undertook a systematic diversification of this compound to identify a 4-(5-phenylthiazole-2-carboxamido)cyclohexanecarboxylic acid scaffold I [R = PhNHCO, 3,5-F2C6H3CO, 3,5-F2C6H3SO2, etc.]. Further linker optimization of this scaffold identified compound I [R = 2-FC6H4NHCO] (DGAT1 IC50 = 14.8 nM) as a potent DGAT1 inhibitor. Coupled with its in vitro potency, the compound also exhibited 112% plasma triglyceride reduction at a 3 mpk dose in an oral fat tolerance test when studied in Swiss mice. After reading the article, we found that the author used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Related Products of 16982-21-1)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Related Products of 16982-21-1
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics