cas 54001-22-8, 2-(4-CHLOROPHENYL)-4-METHYL-1,3-THIAZOLE-5-CARBONYL CHLORIDE | Articles data ｜lookchem

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54001-22-8

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Design, synthesis, and biological evaluation of thiazoles targeting flavivirus envelope proteins
A series of third-generation analogues of methyl 4-(dibromomethyl)-2-(4- chlorophenyl)thiazole-5-carboxylate (1), which had the most potent antiviral activity among the first- and second-generation compounds, have been synthesized and tested against yellow fever virus using a cell-based assay. The compounds were designed with the objectives of improving metabolic stability, therapeutic index, and antiviral potency. The biological effects of C4 and C5 substitution were examined. The methylthio ester and the dihydroxypropylamide analogues had the best antiviral potencies and improved therapeutic indices and metabolic stabilities relative to the parent compound 1.
Mayhoub, Abdelrahman S.,Khaliq, Mansoora,Kuhn, Richard J.,Cushman, Mark
p. 1704 - 1714
(2011/05/05)

Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARα agonists. 1. Discovery of a novel series of potent HDLc raising agents
The peroxisome proliferator activated receptors PPARα, PPARγ, and PPARδ are ligand-activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-density lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARα agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more potent and selective PPARα agonists. Modification of the selective PPARδ agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARα agonism. Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARα and at least 500-fold selectivity versus PPARγ and PPARγ. Compound 25a (GW590735) has been progressed to clinical trials for the treatment of diseases of lipid imbalance.
Sierra, Michael L.,Beneton, Véronique,Boullay, Anne-Bénédict,Boyer, Thierry,Brewster, Andrew G.,Donche, Frédéric,Forest, Marie-Claire,Fouchet, Marie-Hélène,Gellibert, Fran?oise J.,Grillot, Didier A.,Lambert, Millard H.,Laroze, Alain,Le Grumelec, Christelle,Linget, Jean Michel,Montana, Valerie G.,Nguyen, Van-Loc,Nicodème, Edwige,Patel, Vipul,Penfornis, Annie,Pineau, Olivier,Pohin, Danig,Potvain, Florent,Poulain, Géraldine,Ruault, Cécile Bertho,Saunders, Michael,Toum, Jér?me,Xu, H. Eric,Xu, Robert X.,Pianetti, Pascal M.
p. 685 - 695
(2007/10/03)

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Chemical Properties

Melting Point: 180 °C
Boiling Point: 395.6 °C at 760 mmHg
Flash Point:193.1 °C
Density: 1.417 g/cm³
Storage Temp.:Keep Under nitrogen
Vapor Pressure: 1.81E-06mmHg at 25°C
Refractive Index: 1.617
PSA: 58.20000
LogP: 4.15090

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