773875-80-2Relevant academic research and scientific papers
Structural studies of pterin-based inhibitors of dihydropteroate synthase
Hevener, Kirk E.,Yun, Mi-Kyung,Qi, Jianjun,Kerr, Iain D.,Babaoglu, Kerim,Hurdle, Julian G.,Balakrishna, Kanya,White, Stephen W.,Lee, Richard E.
, p. 166 - 177 (2010)
Dihydropteroate synthase (DHPS) is a key enzyme in bacterial folate synthesis and the target of the sulfonamide class of antibacterials. Resistance and toxicities associated with sulfonamides have led to a decrease in their clinical use. Compounds that bi
SELECTIVE GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 34; 42; 48; 51, (2015/06/03)
Described herein are certain steroid derivative compounds, for example of formula (I): wherein X1, X2, X3 L, and Ar are as defined herein, pharmaceutical compositions comprising such compounds, the use of such compounds and compositions to specifically target glucocorticoid action, and the use of such compounds and compositions in the treatment of acute and chronic inflammatory conditions, in particular rheumatoid arthritis, haematological and other malignancies, and for causing immunosuppression in the prevention or treatment of transplant rejection, as well as methods of preparing such compounds.
Synthesis and activities of new arylsulfonamido thromboxane A2 receptor antagonists
Sartori, E.,Camy, F.,Teulon, J. M.,Caussade, F.,Virone-Oddos, A.,Cloarec, A.
, p. 625 - 632 (2007/10/02)
New benzoic, benzeneacetic and thiazole-4-acetic acids bearing an arylsulfonamido alkyl or alkylhetero side chain were synthesized and tested in vitro for affinity for human platelet thromboxane A2 receptors and inhibition of U46619-induced rat aortic ring contraction.Influence of substitution patterns, chain length and presence of heteroatoms were studied and compounds within a 30 nmol range for inhibition of U46619-induced contractions were found.One of the most potent, 2-thiazole-4-acetic acid (VII-4) was orally active (1 mg/kg), as evidenced by the inhibition of U46619-induced platelet aggregation in guinea pigs, ex vivo. thromboxane A2 / receptor antagonist / platelet aggregation / arylsulfonamido derivative
