Discovery of Barakacin and Its Derivatives as Novel Antiviral and Fungicidal Agents

Pesticides are essential for the development of agriculture. It is urgent to develop green, safe and efficient pesticides. Bisindole alkaloids have unique and concise structures and broad biological activities, which make them an important leading skeleton in the creation of new pesticides. In this work, we synthesized bisindole alkaloid barakacin in a simple seven-step process, and simultaneously designed and synthesized a series of its derivatives. Biological activity research indicated that most of these compounds displayed good antiviral activities against tobacco mosaic virus (TMV). Among them, compound 14b exerted a superior inhibitory effect in comparison to commercially available antiviral agent ribavirin, and could be expected to become a novel antiviral candidate. Molecular biology experiments and molecular docking research found that the potential target of compound 14b was TMV coat protein (CP). These compounds also showed broad-spectrum anti-fungal activities against seven kinds of plant fungi.

Automated summary

Pesticides are crucial for agricultural development, and the development of green, safe, and efficient pesticides is urgent. Bisindole alkaloids, with their unique and concise structures and broad biological activities, play an important role in the creation of new pesticides. In this study, bisindole alkaloid barakacin and its derivatives were synthesized and evaluated for their antiviral and antifungal activities. Compound 14b exhibited superior antiviral activity against tobacco mosaic virus (TMV) and could potentially serve as a novel antiviral candidate.