Abstract
A series of 1,3,4-oxadiazole contained sesquiterpene derivatives were synthesized, and the activity of the target compounds against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas axonopodis pv. citri (Xac), and tobacco mosaic virus (TMV) were evaluated. The biological activity results showed that the EC50 values of compounds H4, H8, H11, H12, H14, H16, and H19 for Xac inhibitory activity were 33.3, 42.7, 56.1, 74.5, 37.8, 43.8, and 38.4 μg/ml, respectively. Compounds H4, H8, H15, H19, H22, and H23 had inhibitory effects on Xoo, with EC50 values of 51.0, 43.3, 43.4, 50.5, 74.6, and 51.4 μg/ml, respectively. In particular, the curative and protective activities of compound H8 against Xoo in vivo were 51.9 and 49.3%, respectively. In addition, the EC50 values of the inactivation activity of compounds H4, H5, H9, H10, and H16 against TMV were 69.6, 58.9, 69.4, 43.9, and 60.5 μg/ml, respectively. The results of molecular docking indicated that compound H10 exhibited a strong affinity for TMV-coat protein, with a binding energy of −8.88 kcal/mol. It may inhibit the self-assembly and replication of TMV particles and have an anti-TMV effect, which supports its potential usefulness as an antiviral agent.
Highlights
Most plant diseases are caused by biological agents such as bacteria, fungi, viruses, and nematodes, which have adverse impact on the growth and development of plants (Das et al, 2016)
Compounds H4 and H14 had an inhibitory effect on Xanthomonas axonopodis pv. citri (Xac), with their EC50 values being 33.3 and 37.8 μg/ml, respectively, better than for bismerthiazol (38.2 μg/ml)
The results exhibited that the synthetic compounds had good antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo) and Xac
Summary
Most plant diseases are caused by biological agents such as bacteria, fungi, viruses, and nematodes, which have adverse impact on the growth and development of plants (Das et al, 2016). Rice bacterial blight caused by Xanthomonas oryzae pv. Oryzae (Xoo) seriously threatens the growth and production of rice by affecting the tillering stage of rice (Wang et al, 2021). Pesticides are the main means of controlling crop diseases and insect pests (Kemmitt et al, 2018). For plant disease, such as Xoo, Xac or TMV, there are traditional medicines (such as Bismerthiazol, Thiodiazole copper, Ningnanmycin and Ribavirin), their effectiveness is limited various forms of disease and insect resistance (Buttimer et al, 2017; Liu et al, 2021). Natural products have special structural characteristics and unique biological activity mechanisms, and they are an important source for discovery of highly effective, safe, and environmentally compatible drugs (Zhang et al, 2018; Zheng and Hua, 2020; Li and Wang, 2021)
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