期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 12, 页码 2470-2475出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00449
关键词
Candida auris; Fluconazole; Resistance; 2-Aryloxazoline; L-threonine; alpha-aminoalcohols
资金
- National Council for Scientific and Technological Development (CNPq) [405556/2018-7]
- Sao Paulo Research Foundation (FAPESP) [2017/19374-9, 2018/11612-0]
- Coordination for the Improvement of Higher Education Personnel (CAPES) [001]
- CNPQ [303373/2019-9]
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [18/11612-0] Funding Source: FAPESP
Because of the increased resistance to currently available antifungals, fungal infections represent a significant challenge to human health. Herein, we report the synthesis of 2-aryloxazoline derivatives from the reaction between L-threonine and derivatives of salicylic or naphthoic acid. In total, 26 compounds were obtained and tested against species of Candida, Cryptococcus, and Aspergillus. We found that all of the compounds inhibited the growth of Candida species at low concentrations (<0.25 mu g/mL) and exhibited reduced hemolytic and cytotoxic activities. Additionally, compounds 4i and 9i were especially effective against antifungal-resistant isolates and the emerging fungus Candida auris. However, the compounds were less active on Cryptococcus and Aspergillus. Because of the improved in vitro antifungal efficacy and attenuated cytotoxicity, these two 2-aryloxazolines obtained from salicylic and naphthoic acid derivatives, respectively, may be considered lead molecules for the development of novel antifungal drugs.
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