title: Design, synthesis, and antiviral activities of 1,5-benzothiazepine derivatives containing pyridine moiety.
abstract: In our previous work, a series of novel benzothiazepine derivatives containing pyridine moiety were successfully synthesized through chalcone 1,3-dipolar cycloaddition and determined their antiviral activity against tobacco mosaic virus (TMV). Bioassay results indicated that most of these target compounds exhibited improved curative, protection, and inactivation activity in vivo than the commercial agent ningnanmycin. Particularly, compound 3m exhibited marked curative activity against TMV, with an EC50value of 352.2 μM, which was even better than that of ningnanmycin. The compound was identified as the most promising candidate for inhibiting plant virus and an excellent compound with antiviral activities against TMV. Structure-activity relationship experiment indicated that the 1,5-benzothiazepine moiety is crucial for potent anti-TMV activity.
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, PR China.
authors.forename: Tianxian
authors.initials: T
authors.lastname: Li
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, PR China.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, PR China.
authors.forename: Jianke
authors.initials: J
authors.lastname: Pan
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, PR China.
authors.forename: Zengxue
authors.initials: Z
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, Guizhou University, Huaxi District, Guiyang 550025, PR China.
authors.forename: Deyu
authors.initials: D
authors.lastname: Hu
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, PR China. Electronic address: songbaoan22@yahoo.com.
authors.forename: Baoan
authors.initials: B
authors.lastname: Song
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry; D013329:Structure-Activity Relationship; D013841:Thiazepines / Q000737:chemistry* / Q000494:pharmacology*; D014027:Tobacco Mosaic Virus / Q000187:drug effects*
chemical_list: C106746:1,5-benzothiazepine; D000998:Antiviral Agents; D011725:Pyridines; D013841:Thiazepines
keywords: 1,3-Dipolar cycloaddition; Antiviral activity; Benzothiazepine derivatives; Pyridine