Synthesis and antifungal activities of 3-alkyl substituted thieno[2,3-d]pyrimidinones

[摘要] The 3-aryl substituted thieno[2,3-d]pyrimidinones 3 by sequential reaction of iminophosphorane 1, aromatic isocyanates and various nucleophiles (HY), found some compounds showed good antitumor and antibacterial activities. Meanwhile, aliphatic isocyanates were applied in the reaction to prepare 3-alkyl substituted thieno[2,3- d]pyrimidinones, but there are no reports of their antifungal activities. As a continuation of our research for new biologically active heterocycles, we herein wish to report a facile synthesis and antifungal activities of 3-alkyl substituted thieno[2,3-d]pyrimidinones 6 via easily accessible iminophosphorane 1. The growth inhibitory effect of one concentration (50mg/L) of compounds 6 against five fungus(Fusarium oxysporium, Rhizoctonia solani, Colletotrichum gossypii, Gibberella zeae and Dothiorella gregaria) in vitro was tested by the method of toxic medium. Compound 6d showed the best inhibition rate against Gibberella zeae with 85.68%.

[发布机构] Laboratory of Chinese Herbal Pharmacology, Renmin Hospital, Hubei University of Medicine, Shiyan; 442000, China^1

[效力级别] 生物科学

[关键词] Aliphatic isocyanates;Anti-bacterial activity;Anti-fungal activity;Facile synthesis;Iminophosphoranes;Inhibitory effect;Rhizoctonia solani;Sequential reaction