Structure-activity relationships of novel alkylides: 3-O-Arylalkyl clarithromycin derivatives with improved antibacterial activities was written by Liang, Jian-Hua;Li, Xiao-Li;Wang, He;An, Kun;Wang, Yue-Ying;Xu, Ying-Chun;Yao, Guo-Wei. And the article was included in European Journal of Medicinal Chemistry in 2012.Category: ethers-buliding-blocks This article mentions the following:
A series of novel alkylides, possessing 3-O-arylalkyl group instead of 3-O-cladinose, were designed, synthesized and evaluated for in vitro antibacterial activities. The increased potency clearly ranked by the order of 3-O-(3-aryl-2-propargyl), 3-O-(3-aryl-E-prop-2-enyl), 3-O-(3-aryl-propyl), and 3-O-(3-aryl-Z-prop-1-enyl) groups. Some alkylides, e.g. I, showed improved activities against inducible MLSB resistance and efflux resistance compared to the second-generation macrolides. Among them, I possessed comparable activities against erythromycin-susceptible Staphylococcus aureus, Streptococcus pneumoniae and Streptococcus pyogenes (MICs of 0.016-0.5 μg/mL). Moreover, I displayed dramatically enhanced potency against both efflux resistant and MLSB resistant strains (MICs of 0.125-0.5 μg/mL) resistant to clarithromycin and azithromycin (MICs of 1- >254 μg/mL), independent of methicillin-susceptible and methicillin-resistant pheno-types. In the experiment, the researchers used many compounds, for example, 1,1-Diisopropoxycyclohexane (cas: 1132-95-2Category: ethers-buliding-blocks).
1,1-Diisopropoxycyclohexane (cas: 1132-95-2) belongs to ethers. The oxygen atom in ethers are more electronegative than carbon, thus the hydrogens which are alpha to the ethers are more acidic than the simple hydrocarbons. Autoxidation is the spontaneous oxidation of a compound in air. In the presence of oxygen, ethers slowly autoxidize to form hydroperoxides and dialkyl peroxides. If concentrated or heated, these peroxides may explode. To prevent such explosions, ethers should be obtained in small quantities, kept in tightly sealed containers, and used promptly.Category: ethers-buliding-blocks