Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains was written by Ni, Tingjunhong;Ding, Zichao;Xie, Fei;Hao, Yumeng;Bao, Junhe;Zhang, Jingxiang;Yu, Shichong;Jiang, Yuanying;Zhang, Dazhi. And the article was included in Molecules in 2022.Electric Literature of C4H11NO This article mentions the following:
A series of triazole derivatives containing phenylethynyl pyrazole moiety as side chain I (R = 4-fluorobenzylaminyl, 4-hydroxypiperidin-1-yl, morpholin-4-yl, etc.) and II (R1 = F, Cl, CN, CF3, OCF3) were designed, synthesized, and most of them exhibited good in vitro antifungal activities. Especially, triazole derivatives I (R = (furan-2-ylmethyl)aminyl) and II (R1 = CN) showed excellent in vitro activities against C. albicans (MIC = 0.125, 0.0625μg/mL), C. neoformans (MIC = 0.125, 0.0625μg/mL), and A. fumigatus (MIC = 8.0, 4.0μg/mL). Triazole derivatives II (R1 = CN) also exerted superior activity to triazole derivatives I (R = (furan-2-ylmethyl)aminyl) and fluconazole in inhibiting hyphae growth of C. albicans and inhibiting drug-resistant strains of C. albicans, and it could reduce fungal burdens in mice kidney at a dosage of 1.0 mg/kg. An in vivo efficacy evaluation indicated that triazole derivatives II (R1 = CN) could effectively protect mice models from C. albicans infection at doses of 0.5, 1.0, and 2.0 mg/kg. These results suggested that triazole derivatives II (R1 = CN) deserves further investigation. In the experiment, the researchers used many compounds, for example, (R)-2-Aminobutan-1-ol (cas: 5856-63-3Electric Literature of C4H11NO).
(R)-2-Aminobutan-1-ol (cas: 5856-63-3) belongs to alcohols. Under appropriate conditions, inorganic acids also react with alcohols to form esters. To form these esters, a wide variety of specialized reagents and conditions can be used. A multistep synthesis may use Grignard-like reactions to form an alcohol with the desired carbon structure, followed by reactions to convert the hydroxyl group of the alcohol to the desired functionality.Electric Literature of C4H11NO
Referemce:
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