Shen, Lan published the artcileSynthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors α/δ dual agonists, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Bioorganic & Medicinal Chemistry (2008), 16(6), 3321-3341, database is CAplus and MEDLINE.
Replacement of the methyl-thiazole moiety of GW501516 (a PPARδ selective agonist) with [1,2,4]thiadiazole gave compound 21 (I) which unexpectedly displayed submicromolar potency as a partial agonist at PPARα in addition to the high potency at PPARδ. A structure-activity relationships study of 21 resulted in the identification of 40 as a potent and selective PPARα/δ dual agonist. Compound 40 and its close analogs represent a new series of PPARα/δ dual agonists. The high potency, high selectivity, significant gene induction, excellent PK profiles, low P 450 inhibition or induction, and good in vivo efficacy in four animal models support 40 being selected as a pre-clin. study candidate, and may render 40 as a valuable pharmacol. tool in elucidating the complex roles of PPARα/δ dual agonists, and the potential usage for the treatment of metabolic syndrome.
Bioorganic & Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C30H32ClN7O2, Recommanded Product: 2,4-Dichlorobenzamide.
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https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics