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Design, synthesis, and antiviral activities of 1,5-benzothiazepine derivatives containing pyridine moiety
Ist Teil von
European journal of medicinal chemistry, 2017-01, Vol.125, p.657-662
Ort / Verlag
France: Elsevier Masson SAS
Erscheinungsjahr
2017
Link zum Volltext
Quelle
Elsevier ScienceDirect Journals Complete
Beschreibungen/Notizen
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 EC50 value 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.
A series of novel benzothiazepine derivatives containing pyridine moiety were synthesized and screened for their antiviral activity against TMV in vivo. [Display omitted]
•Benzothiazepine were synthesized through 1,3-dipolar cycloaddition.•Compound 3m exhibited marked curative activity against TMV.•Electron-withdrawing groups are in favors of antiviral activity.