[EN] THIAZOLE DERIVATIVES AS SGLT2 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME [FR] DÉRIVÉS DE THIAZOLE EN TANT QU'INHIBITEURS DE SGLT2 ET COMPOSITION PHARMACEUTIQUE COMPRENANT CEUX-CI
[EN] PHOSPHONIC ACID DERIVATES AND THEIR USE AS P2Y12 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS D'ACIDE PHOSPHONIQUE ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DU RÉCEPTEUR P2Y12
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2009069100A1
公开(公告)日:2009-06-04
The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).
New greenfluorescentprotein (GFP) chromophoreanalogues, namely 4-(diarylmethylene)imidazolinones (DAINs), were readily synthesized under weakly acidic conditions using a novel condensation reaction between methyl imidate (or thioimidate) and ethyl N-(diarylmethylene)glycinate. DAINs showed notable fluorescence properties. Although they were nearly non-fluorescent in the solution, visible emissions
The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
Synthesis and antimicrobial activities of novel sorbic and benzoic acid amide derivatives
作者:Qingyi Wei、Xiaomei Wang、Jun-Hu Cheng、Guangxiang Zeng、Da-Wen Sun
DOI:10.1016/j.foodchem.2018.06.071
日期:2018.12
sorbic and benzoicacid amide derivatives were synthesized by conjugating sorbic acid (SAAD, a1–a7) or benzoicacid (BAAD b1–b6) with amino acid esters and their antimicrobial activities were investigated against Escherichia coli, Bacillus subtilis and Staphylococcus aureus, mixed bacteria from rancid milk, Saccharomyces cerevisiae, and Aspergillus niger. The antimicrobial activity of sorbic acid amides
通过将山梨酸(SAAD,a 1 – a 7)或苯甲酸(BAAD b 1 – b 6)与氨基酸酯缀合来合成一系列山梨酸和苯甲酰胺衍生物,并研究了它们对大肠杆菌,芽孢杆菌的抗菌活性。枯草芽孢杆菌和金黄色葡萄球菌,腐乳,酿酒酵母和黑曲霉中的混合细菌。山梨酰胺的抗菌活性优于苯甲酰胺。化合物的最小抑制浓度(MIC)异丙基N- [1-氧代-2,4-己二烯-1-基] -L-苯基丙氨酸甲酯(一个7)为0.17毫针对枯草芽孢杆菌,和0.50毫摩尔对金黄色葡萄球菌,而山梨酸的MIC值分别大于2 mM。同样,化合物a 7在pH 5.0-9.0的范围内表现出与pH无关的抗菌活性,并且在pH 9.0时有效。这些结果表明,山梨酸与氨基酸酯的缀合导致体外显着改善。 抗菌特性,但对苯甲酰胺衍生物几乎没有观察到作用。