Abstract
A series of myricetin derivatives containing amide, thioether, and 1,3,4-thiadiazole moieties were designed and synthesized, and their antiviral and antibacterial activities were assessed. The bioassays showed that all the title compounds exhibited potent in vitro antibacterial activities against Xanthomonas citri (Xac), Ralstonia solanacearum (Rs), and Xanthomonas oryzae pv. Oryzae (Xoo). In particular, the compounds 5a, 5f, 5g, 5h, 5i, and 5l, with EC50 values of 11.5–27.3 μg/mL, showed potent antibacterial activity against Xac that was better than the commercial bactericides Bismerthiazol (34.7 μg/mL) and Thiodiazole copper (41.1% μg/mL). Moreover, the in vivo antiviral activities against tobacco mosaic virus (TMV) of the target compounds were also tested. Among these compounds, the curative, protection, and inactivation activities of 5g were 49.9, 52.9, and 73.3%, respectively, which were better than that of the commercial antiviral Ribavirin (40.6, 51.1, and 71.1%, respectively). This study demonstrates that myricetin derivatives bearing amide, thioether, and 1,3,4-thiadiazole moieties can serve as potential alternative templates for the development of novel, highly efficient inhibitors against plant pathogenic bacteria and viruses.
Highlights
IntroductionNatural products and extracts, derived from the biosphere, have been widely applied for use in medicines [2], pesticides [3,4], cosmetics [5], and food products in ancient and modern societies around the world [6]
In recent years, pathogenic bacteria and plant viruses targeting agricultural crops have become increasingly difficult to control, leading to enormous losses in worldwide crop production each year.As such, the development of environmentally friendly pesticides with high selectivity, high efficiency, low toxicity, and suitable degradation are important challenges to both chemists and biologists [1].Natural products and extracts, derived from the biosphere, have been widely applied for use in medicines [2], pesticides [3,4], cosmetics [5], and food products in ancient and modern societies around the world [6]
2-amino-5-mercaptoThe synthesis protocol was divided into five steps (Scheme 1)
Summary
Natural products and extracts, derived from the biosphere, have been widely applied for use in medicines [2], pesticides [3,4], cosmetics [5], and food products in ancient and modern societies around the world [6]. Many natural products have shown promise as antimicrobials and antivirals [7], including the quercetin, genistein, and silybin, which belong to the flavonoids group of compounds and have demonstrated inhibitory activity against the DNA virus herpes type 1 (HSV-1) and RNA virus parainfluenza type 3 (PI-3) [8]. Myricetin (Figure 1) belongs to a class of natural flavonoids that is widely found in vegetables, fruits, teas, and medicine herbs [9,10].
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