title: Synthesis and antiviral activity of 2-substituted methylthio-5-(4-amino-2-methylpyrimidin-5-yl)-1,3,4-oxadiazole derivatives.
abstract: A series of novel 2-substituted methylthio-5-(4-amino-2-methylpyrimidin-5-yl-)-1,3,4-oxadiazole derivatives were synthesized and evaluated for antiviral activities against tobacco mosaic virus (TMV) via half-leaf method. The preliminary biological results showed that these compounds exhibited good antiviral activity against TMV in vivo. Among these compounds, compounds 8f, 8h, 8k, 8n, 8q and 8w exhibited the similar curative effect against TMV (EC50=290.98-438.29μg/mL) as the commercial product Ningnanmycin (301.83μg/mL). Notably, compound 8i exhibited the excellent curative effect against TMV, with EC50 value of 246.48μg/mL, which was better than that of Ningnanmycin. To the best of our knowledge, this was the first Letter of 2-substituted methylthio-5-(4-amino-2-methylpyrimidin-5-yl-)-1,3,4-oxadiazole derivatives with potent antiviral against TMV.
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
authors.forename: Wenneng
authors.initials: W
authors.lastname: Wu
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
authors.forename: Qin
authors.initials: Q
authors.lastname: Chen
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
authors.forename: Anqi
authors.initials: A
authors.lastname: Tai
authors.affiliation: College of Chemistry and Chemical Engineering, Guizhou University, Guiyang 550025, PR China.
authors.forename: Guangqi
authors.initials: G
authors.lastname: Jiang
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China. Electronic address: oygp710@163.com.
authors.forename: Guiping
authors.initials: G
authors.lastname: Ouyang
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D018360:Crystallography, X-Ray; D003562:Cytidine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014027:Tobacco Mosaic Virus / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D010069:Oxadiazoles; C000594254:ningnanmycin; C583463:1,3,4-oxadiazole; D003562:Cytidine
keywords: 1,3,4-Oxadiazole; 4-Amino-2-methylpyrimidine moiety; Antiviral activity; Synthesis; Tobacco mosaic virus