Roedl, Carmen B. published the artcileMulti-dimensional target profiling of N,4-diaryl-1,3-thiazole-2-amines as potent inhibitors of eicosanoid metabolism, Recommanded Product: 1-(4-Chlorophenyl)thiourea, the publication is European Journal of Medicinal Chemistry (2014), 302-311, database is CAplus and MEDLINE.
Eicosanoids like leukotrienes and prostaglandins play a considerable role in inflammation. Produced within the arachidonic acid (AA) cascade, these lipid mediators are involved in the pathogenesis of pain as well as acute and chronic inflammatory diseases like rheumatoid arthritis and asthma. With regard to the lipid cross-talk within the AA pathway, a promising approach for an effective anti-inflammatory therapy is the development of inhibitors targeting more than one enzyme of this cascade. Within this study, thirty N-4-diaryl-1,3-thiazole-2-amine based compounds with different substitution patterns were synthesized and tested in various cell-based assays to investigate their activity and selectivity profile concerning five key enzymes involved in eicosanoid metabolism (5-, 12-, 15-lipoxygenase (LO), cyclooxygenase-1 and -2 (COX-1/-2)). With compound ST-1355, 2-(4-phenylthiazol-2-ylamino)phenol, a multitarget ligand targeting all tested enzymes is presented, whereas compound ST-1705, 2-(4-(4-chlorophenyl)thiazol-2-ylamino)phenol, represents a potent and selective 5-LO and COX-2 inhibitor with an IC50 value of 0.9±0.2 μM (5-LO) and a residual activity of 9.1±1.1% at 10 μM (COX-2 product formation). The promising characteristics and the addnl. noncytotoxic profile of both compounds reveal new lead structures for the treatment of eicosanoid-mediated diseases.
European Journal of Medicinal Chemistry published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Recommanded Product: 1-(4-Chlorophenyl)thiourea.
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