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.Related Products of 65705-44-4.Hanke, Thomas; Dehm, Friederike; Liening, Stefanie; Popella, Sven-Desiderius; Maczewsky, Jonas; Pillong, Max; Kunze, Jens; Weinigel, Christina; Barz, Dagmar; Kaiser, Astrid; Wurglics, Mario; Laemmerhofer, Michael; Schneider, Gisbert; Sautebin, Lidia; Schubert-Zsilavecz, Manfred; Werz, Oliver published the article 《Aminothiazole-Featured Pirinixic Acid Derivatives As Dual 5-Lipoxygenase and Microsomal Prostaglandin E2 Synthase-1 Inhibitors with Improved Potency and Efficiency in Vivo》 about this compound( cas:65705-44-4 ) in Journal of Medicinal Chemistry. Keywords: aminothiazole pirinixic acid preparation Lipoxygenase mPGES1 inhibitory activity. Let’s learn more about this compound (cas:65705-44-4).
Dual inhibition of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO) is currently pursued as potential pharmacol. strategy for treatment of inflammation and cancer. Here we present a series of 26 novel 2-aminothiazole-featured pirinixic acid derivatives as dual 5-LO/mPGES-1 inhibitors with improved potency (exemplified by compound 2-[(4-chloro-6-{[4-(naphthalen-2-yl)-1,3-thiazol-2-yl]-amino}-pyrimidin-2-yl)-sulfanyl]-octanoic acid (I) with IC50 = 0.3 and 0.4 μM, resp.) and bioactivity in vivo. Computational anal. presumes binding sites of I at the tip of the 5-LO catalytic domain and within a subpocket of the mPGES-1 active site. Compound I (10 μM) hardly suppressed cyclooxygenase (COX)-1/2 activities, failed to inhibit 12/15-LOs, and is devoid of radical scavenger properties. Finally, compound I reduced vascular permeability and inflammatory cell infiltration in a zymosan-induced mouse peritonitis model accompanied by impaired levels of cysteinyl-leukotrienes and prostaglandin E2. Together, 2-aminothiazole-featured pirinixic acids represent potent dual 5-LO/mPGES-1 inhibitors with an attractive pharmacol. profile as anti-inflammatory drugs.
As far as I know, this compound(65705-44-4)Related Products of 65705-44-4 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.
Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics