Design, Synthesis and Biological Activities of Novel N-Aryl-1H-pyrazole-5-carboxylate Derivatives

Abstract

In an attempt to search for potent fungicide, a series of novel N-aryl-1H-pyrazole-5-carboxylate derivatives was designed and synthesized. Their chemical structures were characterized by ¹H NMR spectra and high resolution mass spectrometry(HRMS). The preliminary bioassay results indicated that some target compounds displayed better fungicidal activities against certain fungi at 50 µg/mL or favorable antitumor activities at 5 µg/mL compared with chlorothalonil and 5-fluorouracil, respectively. The structure-activity relationship demonstrated that the introduction of ester group and amide bond was favorable to the improvement of activities against Physalospora piricola and Phytophthora capsici.

Keywords

N-Aryl-1H-pyrazole-5-carboxylate / Fungicidal activity / Antitumor activity

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