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

Abstract

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.

Discovery of Novel Oxathiapiprolin Derivatives as Potent Fungicide Candidates

“…Our previous study showed that the binding site space for the pyrazole group in OXA could accommodate larger molecular fragments. As we know, the indole ring is a functional and versatile fragment that has been widely applied in drug and pesticide design. − Some of representative compounds ( compound 15–31 − containing the indole ring are shown in Figure S1. Here, to continue our research on OXA, an indole fragment was introduced into OXA to replace the pyrazole ring (Figure ).…”