Design, Synthesis, Antifungal Activity and Molecular Docking of Thiochroman-4-one Derivatives

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  • Zhong Yifan
    Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University
  • Han Xiaoyan
    Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University
  • Li Shengbin
    Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University
  • Qi Hui
    Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University
  • Song Yali
    Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University
  • Qiao Xiaoqiang
    Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University

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<p>N-Myristoyltransferase (NMT) has been validated pre-clinically as a target for treatment of fungal infections. Various substituted thiochroman-4-one derivatives have been synthesized by an efficient method. The synthesized compounds 7a–y and 8a–t were evaluated for their in vitro antifungal activity against the Canidia albicans, Cryptococcus neoformans, Epidermophyton floccosum, Mucor racemosus, Microsporum gypseum and Aspergillus nigerstrain. A series of compounds exhibited significant activity (minimal inhibitory concentrotion (MIC)=0.5–16 µg/mL) against Canidia albicans and Cryptococcus neoformans. The antifungal activity of compound 7b was reached to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the NMT inhibitors. The molecular docking studies revealed an interesting binding profile with very high receptor affinity for NMT of Canidia albicans.</p>

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