【摘 要】
：
A series of structurally novel 1,3,4-oxadiazole thioether derivatives (6a-6z) containing a 6-fluoroquinazolinylpiperidinyl moiety were designed and synthesized
【机 构】
：
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laborator
论文部分内容阅读
A series of structurally novel 1,3,4-oxadiazole thioether derivatives (6a-6z) containing a 6-fluoroquinazolinylpiperidinyl moiety were designed and synthesized using pharmacophore hybrid approach, and their structures were fully characterized by 1H NMR, 13C NMR and HRMS spectra. Among them, the structure of compound 6d was further corroborated via single-crystal X-ray diffraction analysis. In vitro antibacterial bioassays showed that compounds 6a, 6g, 6u and 6v possessed EC50 values of 30.4, 30.6, 27.5 and 26.0μg/mL against phytopathogenic bacterium Xanthomonas oryzae pv. oryzae, respectively, which were significantly superior to that of commercially-available bactericide Bismerthiazol (85.1μg/mL). Moreover, in vitro antifungal bioassays indicated that seven compounds demonstrated broad-spectrum fungicidal acitivties against six types of phytopathogenic fungi at 50μg/mL. The present work showed the potential of 1,3,4-oxadiazole thioether derivatives carrying a 6-fluoroquinazolinylpiperidinyl moiety as effective antimicrobial agents for crop protection, deserving further investigations in the future.
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