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Design, synthesis and antifungal activity of novel selenochroman-4-one derivatives

Hang Xu, Yu-Kun Hu, Meng-Bi Guo, Ai-Su Huang, Xin Su, and Chun Guo

Shenyang Pharmaceutical University, Shenyang, China

 

E-mail: suxin1966@163.com

Abstract: A series of novel selenochroman-4-one derivatives bearing semicarbazone or nitrogen heterocycle was designed, synthesized, tested antifungal activity and characterized via 1H-NMR, 13C-NMR, and HRMS. The design of the compounds is based on the principle of molecule hybrid and bioisosterism. We aimed at attaching semicarbazones or nitrogen heterocycle to the selenochroman-4-one for enhancing antifungal activity. The antifungal activity of target compounds was evaluated using the microdilution broth method in vitro test. Bioassay results indicated that some of the derivatives displayed good fungistatic activity on Candida zeylanoides, Candida albicans, Cryptococcus neoformans, resistant to fluconazole strain 103 (Candida albicans), resistant to fluconazole strain 100 (Candida albicans) and strain SC5314 (Candida albicans). All the compounds exhibit antifungal activities against the tested funguses in different levels, among them, 7 compounds of antifungal activity against several funguses is better than that of the control drug fluconazole. Based on the results, preliminary structure activity relationships (SARs) were summarized to serve as a foundation for further investigation.

Keywords: Selenochroman-4-one; Synthesis; Antifungal activity; Bioisosterism; Molecule hybrid

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-017-0239-z

 

Chemical Papers 71 (12) 2455–2463 (2017)

Sunday, July 12, 2020

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