On January 7, 2015, Lill, Andreas P.; Roedl, Carmen B.; Steinhilber, Dieter; Stark, Holger; Hofmann, Bettina published an article.Computed Properties of 27115-50-0 The title of the article was Development and evaluation of ST-1829 based on 5-benzylidene-2-phenylthiazolones as promising agent for anti-leukotriene therapy. And the article contained the following:
Different inflammatory diseases and allergic reactions are mediated by leukotrienes, which arise from the oxygenation of arachidonic acid catalyzed by 5-lipoxygenase (5-LO). One promising approach for an effective anti-leukotriene therapy (leukotriene antagonists) is the inhibition of this key enzyme. This study presents the synthesis and development of a potent and direct 5-LO inhibitor based on the well characterized 5-benzylidene-2-phenylthiazolone C06, whose further pharmacol. investigation was precluded due to its low solubility Through optimization of C06, evaluation of a structure-activity relationship including profound assessment of the thiazolone core and consideration of the solubility, the 5-benzyl-2-phenyl-4-hydroxythiazoles represented by ST-1829 [i.e., 5-(4-chlorobenzyl)-2-p-tolyl-4-thiazolol] were developed. ST-1829 showed an improved 5-LO inhibitory activity in cell-based (IC50 values 0.14 μM) and cell-free assays (IC50 values 0.03 μM) as well as a prominent enhanced solubility Furthermore, ST-1829 kept its promising inhibitory potency in the presence of blood serum, excluding excessive binding to serum proteins. These facts combined with the non-cytotoxic profile mark a major step towards an effective anti-inflammatory therapy. The synthesis of the target compounds was achieved using 2-thioxo-4-thiazolidinone, 4-methylbenzoic acid, aldehydes, nitriles as simple starting materials. The title compounds thus formed included 2-(4-chlorophenyl)-5-[(4-methoxyphenyl)methyl]-4-thiazolol, 5-[(4-methoxyphenyl)methylene]-2-(4-methylphenyl)-4-thiazolone and related substances. Analogs included (3E)-3-[(4-methoxyphenyl)methylene]-5-(4-methylphenyl)-2(3H)-furanone, (4Z)-4-[(4-methoxyphenyl)methylene]-2-(4-methylphenyl)-5(4H)-oxazolone. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Computed Properties of 27115-50-0
The Article related to thiazole thiazolone thiazolol preparation leukotriene antagonist, 5-lipoxygenase, anti-leukotriene therapy, hydroxythiazoles, inflammation, solubility, structure–activity relationship and other aspects.Computed Properties of 27115-50-0
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