Category: ethers-buliding-blocksIn 2019 ,《Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives》 appeared in European Journal of Medicinal Chemistry. The author of the article were Zhu, Wen-Jing; Cui, Ben-Wen; Wang, Hui Min; Nan, Ji-Xing; Piao, Hu-Ri; Lian, Li-Hua; Jin, Cheng Hua. The article conveys some information:
Six series of 4-(benzo[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methylpyridin-2-yl)- pyrazoles and 3(5)-(6-methylpyridin-2-yl)-4-(thieno[3,2,-c]- pyridin-2-yl)pyrazoles have been synthesized and evaluated for their activin receptor-like kinase 5 (ALK5) and p38α mitogen activated protein (MAP) kinase inhibitory activities in enzymic assays. Among these compounds, the most active compound, I, inhibited ALK5 phosphorylation with an IC50 value of 0.030 μM in the enzymic assay. Compound I showed four-fold more potent activity against ALK5 kinase than the clin. candidate, compound LY-2157299. The selectivity index of I against p38α MAP kinase is 235, which is much higher than that of LY-2157299 (II) and equally selective to that of EW-7197 (III). Compound I effectively suppressed protein and mRNA expression of collagen I and α-SMA in TGF-β-induced LX-2 human hepatic stellate cell (HSC), this result shows that compound I has the ability to inhibit the activation of HSC. Compound I is expected to be a preclin. candidate for the treatment of hepatic fibrosis. The experimental part of the paper was very detailed, including the reaction process of N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5Category: ethers-buliding-blocks)
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Category: ethers-buliding-blocks
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem