Research speed reading in 2021. Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. Category: Benzisoxazole, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction. 57-11-4, Name is Stearic acid, molecular formula is C18H36O2. In an article, author is Mahindroo, N,once mentioned of 57-11-4.
The synthesis and structure-activity relationship studies of novel indole derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Indole, a druglike scaffold, was studied as a core skeleton for the acidic head part of PPAR agonists. The structural features (acidic head, substitution on indole, and linker) were optimized first, by keeping benzisoxazole as the tail part, based on binding and functional activity at PPAR gamma protein. The variations in the tail part, by introducing various heteroaromatic ring systems, were then studied. In vitro evaluation led to identification of a novel series of indole compounds with a benzisoxazole tail as potent PPAR agonists with the lead compound 14 (BPR1H036) displaying an excellent pharmacokinetic profile in BALB/c mice and an efficacious glucose lowering activity in KKA(y) mice. Structural biology studies of 14 showed that the indole ring contributes strong hydrophobic interactions with PPAR gamma and could be an important moiety for the binding to the protein.
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Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics