The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 8-Bromooctan-1-ol( cas:50816-19-8 ) is researched.Computed Properties of C8H17BrO.Wang, Xin; Liu, Jun; Chen, Jinyao; Zhang, Ming; Tian, Chuan; Peng, Xiaoping; Li, Gang; Chang, Wenqiang; Lou, Hongxiang published the article 《Azole-triphenylphosphonium conjugates combat antifungal resistance and alleviate the development of drug-resistance》 about this compound( cas:50816-19-8 ) in Bioorganic Chemistry. Keywords: azole triphenylphosphonium preparation antifungal fungal infection; Azole-resistance; Candida; Erg11; Fluconazole; Mitochondria-targeting. Let’s learn more about this compound (cas:50816-19-8).
Azole antifungals are commonly used to treat fungal infections but have resulted in the occurrence of drug resistance. Therefore, developing azole derivatives (AZDs) that can both combat established drug-resistant fungal strains and evade drug resistance is of great importance. In this study, we synthesized a series of AZDs with a fluconazole (FLC) skeleton conjugated with a mitochondria-targeting triphenylphosphonium cation (TPP+). These AZDs displayed potent activity against both azole-sensitive and azole-resistant Candida strains without eliciting obvious resistance. Moreover, two representative AZDs, I and II, exerted synergistic antifungal activity with Hsp90 inhibitors against C. albicans strains resistant to the combination treatment of FLC and Hsp90 inhibitors. AZD 25, which had minimal cytotoxicity, was effective in preventing C. albicans biofilm formation. Mechanistic investigation revealed that AZD II inhibited the biosynthesis of the fungal membrane component ergosterol and interfered with mitochondrial function. Our findings provide an alternative approach to address fungal resistance problems.
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