Xu, Hang; Yan, Zhong-zuo; Guo, Meng-bi; An, Ran; Wang, Xin; Zhang, Rui; Mou, Yan-hua; Hou, Zhuang; Guo, Chun published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Lead optimization generates selenium-containing miconazole CYP51 inhibitors with improved pharmacological profile for the treatment of fungal infections》.Application In Synthesis of 1-Bromo-3-methoxybenzene The article contains the following contents:
A series of selenium-containing miconazoles. compounds I, II [R = H, 3-F, 2-Me, etc. ; X= F, Cl], III [R = H, 3-F, 2-Me, etc.; X= F, C] were identified as potent antifungal drugs in our previous study. Representative compound I (MIC = 0.01μg/mL against C.alb. 5314) proved efficacious in inhibiting the growth of fungal pathogens. However, further study showed lead compound I exhibited potential hemolysis, significant cytotoxic effect and unfavorable metabolic stability and was therefore modified to overcome these drawbacks. In this article, the further optimization of selenium-containing miconazole derivatives resulted in the discovery of similarly potent compound II [R = 4-F ; X= F] (MIC = 0.02μg/mL against C.alb. 5314), exhibiting a superior pharmacol. profile with decreased rate of metabolism, cytotoxic effect and hemolysis. Furthermore, compound II [R = 4-F ; X= F] showed fungicidal activity against Candida albicans and significant effects on the treatment of resistant Candida albicans infections. Meanwhile, compound II [R = 4-F ; X= F] not only could reduce the ergosterol biosynthesis pathway by inhibiting CYP51, but also inhibited biofilm formation. More importantly, compound II [R = 4-F ; X= F] also shows promising in vivo efficacy after i.p. injection and the PK study of compound II [R = 4-F ; X= F] was evaluated. In addition, mol. docking studies provide a model for the interaction between the compound II [R = 4-F ; X= F] and the CYP51 protein. Overall, it was believed that these selenium-containing miconazole compounds can be further developed for the potential treatment of fungal infections. After reading the article, we found that the author used 1-Bromo-3-methoxybenzene(cas: 2398-37-0Application In Synthesis of 1-Bromo-3-methoxybenzene)
1-Bromo-3-methoxybenzene(cas: 2398-37-0) is a compound useful in organic synthesis and other chemical processes. It is an intermediate used for pharmaceuticals, perfumes and agrochemicals.Application In Synthesis of 1-Bromo-3-methoxybenzene
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