Yu, Tao published the artcileDiscovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model, Category: iodides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(10), 1686-1692, database is CAplus and MEDLINE.
Diacylglycerol acetyltransferase (DGAT) is expressed abundantly in intestine, liver, and adipose tissues. DGAT1 is the crucial and rate-limiting enzyme that mediates the final step in triacylglycerol (TAG) resynthesis during dietary fat absorption. However, too much triacylglycerol (TAG) reserve will lead to genetic obesity (Hubert et al., 2000). DGAT1 knockout mice could survive and displayed a reduction in the postprandial rise of plasma TG, and increased sensitivity of insulin and leptin. Here the authors report the discovery and characterization of a novel selective DGAT1 inhibitor 29 (5-(4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4f][1,4] oxazepin-6(5H)-yl)-2,6-dimethylphenyl)-3,3-dimethylpent-4-ynoic acid) to potentially treat obesity. Compound 29 showed lipid lowering effect in mouse lipid tolerance test (LTT) and also reduced body weight in DIO mice without observable liver damage.
Bioorganic & Medicinal Chemistry Letters published new progress about 364-12-5. 364-12-5 belongs to iodides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,Iodide,Benzene, name is 5-Bromo-2-iodobenzotrifluoride, and the molecular formula is C3H6O2, Category: iodides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com