An, Yunfei; Liu, Wenxia; Xie, Honglei; Fan, Haiyan; Han, Jun; Sun, Bin published an article on January 5 ,2022. The article was titled 《Construction and activity evaluation of novel benzodioxane derivatives as dual-target antifungal inhibitors》, and you may find the article in European Journal of Medicinal Chemistry.Electric Literature of C10H14ClNO2 The information in the text is summarized as follows:
Ergosterol exert the important function in maintaining the fluidity and osmotic pressure of fungal cells, and its key biosynthesis enzymes (squalene epoxidase, SE; 14 α-demethylase, CYP51) displayed the obvious synergistic effects. Therefore, authors expected to discover the novel antifungal compounds with dual-target (SE/CYP51) inhibitory activity. In the progress, authors screened the different kinds of potent fragments based on the dual-target features, and the method of fragment-based drug discovery (FBDD) was used to guide the construction of three different series of benzodioxane compounds Subsequently, their chem. structures were synthesized and evaluated. These compounds displayed the obvious biol. activity against the pathogenic fungal strains. Notably, (R)-N-(1-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-yl)-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamide and N-((S)-3-methyl-1-oxo-1-(((R)-1-phenyl-2-(1H-1,2,4-triazol-1-yl)ethyl)amino)butan-2-yl)-2,3-dihydrobenzo[b] [1,4]dioxine-5-carboxamide possessed the excellent broad-spectrum anti-fungal activity (MIC50, 0.125-2.0μg/mL) and the activity against drug-resistant strains (MIC50, 0.5-2.0μg/mL). Preliminary mechanism studies have confirmed that these compounds effectively inhibited the dual-target activity, they could cause fungal rupture and death by blocking the bio-synthetic pathway of ergosterol. Further experiments discovered that above compounds also maintained a certain of anti-fungal effect in vivo. The experimental part of the paper was very detailed, including the reaction process of H-Phg-OEt.HCl(cas: 59410-82-1Electric Literature of C10H14ClNO2)
H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. Electric Literature of C10H14ClNO2
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics