In 2019,European Journal of Medicinal Chemistry included an article by Zhao, Liyu; Sun, Nannan; Tian, Linfeng; Sun, Yin; Chen, Yixuan; Wang, Xinran; Zhao, Shizhen; Su, Xin; Zhao, Dongmei; Cheng, Maosheng. Name: (3-Fluorophenyl)boronic acid. The article was titled 《Combating fluconazole-resistant fungi with novel β-azole-phenylacetone derivatives》. The information in the text is summarized as follows:
A series of β-azole-phenylacetone derivatives I (R1 = H, 2-F, 3-F, etc. ; R2 = 2-CH3, 4-F, 2-Cl, etc.; R3 = 3-Cl, 4-F, 4-CH3, etc.) with novel structures were designed and synthesized to combat the increasing incidence of susceptible fungal infections and drug-resistant fungal infections. The antifungal activity of the synthesized compounds was assessed against five susceptible strains and five fluconazole-resistant strains and most of the compounds exhibited excellent antifungal activities with MIC values in the range of 0.03-1 μg/mL. Compounds I (R1 = 3-F, R2 = R3 = H), I (R1 = R2 = H; R3 = 2-F) and I (R1 = 2-F; R2 = H; R3 = 4-CH3) exhibited moderate antifungal activities against fluconazole-resistant strains 17# and CaR with MIC values in the range of 1-8 μg/mL. Compounds I (R1 = 2-F; R2 = R3 = H), I (R1 = R2 = H; R3 = 2-F) and I (R1 = R3 = 2-F; R2 = H) displayed moderate to good antifungal activity against fluconazole-resistant strains 632, 901 and 904 with MIC values in the range of 0.125-4 μg/mL. Notably, I (R1 = R2 = H; R3 = 2-F) and I (R1 = 2-F; R2 = H; R3 = 4-CH3) exhibited antifungal activity against five susceptible strains and five fluconazole-resistant strains. Preliminary mechanistic studies showed that the potent antifungal activity of compound I (R1 = 2-F; R2 = H; R3 = 4-CH3) stemmed from inhibition of C. albicans CYP51. Compounds I (R1 = R2 = H; R3 = 2-F), I (R1 = 3-F; R2 = H; R3 = 4-F) and I (R1 = 2-F; R2 = H; R3 = 4-CH3) were nearly nontoxic to mammalian A549 cells. In the experiment, the researchers used (3-Fluorophenyl)boronic acid(cas: 768-35-4Name: (3-Fluorophenyl)boronic acid)
(3-Fluorophenyl)boronic acid(cas: 768-35-4) can be used to make novel liquid crystalline fluorobiphenylcyclohexenes and difluoroterphenyls by palladium-catalyzed cross-couplings also used in the synthesis of o-phenylphenols as potent leukotriene B4 receptor agonists.Name: (3-Fluorophenyl)boronic acid
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics