The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine( cas:65705-44-4 ) is researched.Quality Control of 4-(4-Bromophenyl)-5-methylthiazol-2-amine.Hanke, Thomas; Lamers, Christina; Gomez, Roberto Carrasco; Schneider, Gisbert; Werz, Oliver; Schubert-Zsilavecz, Manfred published the article 《Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition》 about this compound( cas:65705-44-4 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: preparation pirinixic acid derivative aminothiazole PPAR 5LO mPGES1 cancer; 5-LO; Cancer; Inflammation; PPARα; PPARγ; mPGES-1. Let’s learn more about this compound (cas:65705-44-4).
The concept of dual PPARα/γ activation was originally proposed as a new approach for the treatment of the metabolic syndrome. However, recent results indicated that PPARα as well as PPARγ activation might also be beneficial in the treatment of inflammatory diseases and cancer. We have recently identified aminothiazole-featured pirinixic acids as dual 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors. Here we present the structure-activity relationship of these aminothiazole-featured pirinixic acids as dual PPARα/γ agonists and discuss their advantages with their potential as dual 5-LO/mPGES-1 inhibitors in inflammatory and cancer diseases. Various pirinixic acid derivatives had already been identified as dual PPARα/γ agonists. However, within this series of aminothiazole-featured pirinixic acids we were able to identify the most potent selective PPARγ agonistic pirinixic acid derivative (compound 13, (2-[(4-chloro-6-{[4-(naphthalen-2-yl)-1,3-thiazol-2-yl]amino}pyrimidin-2-yl)sulfanyl]octanoic acid)). Therefore, docking of 13 on PPARγ was performed to determine the potential binding mode.
Although many compounds look similar to this compound(65705-44-4)Quality Control of 4-(4-Bromophenyl)-5-methylthiazol-2-amine, numerous studies have shown that this compound(SMILES:NC1=NC(C2=CC=C(Br)C=C2)=C(C)S1), has unique advantages. If you want to know more about similar compounds, you can read my other articles.
Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics