No abstract

Novel pyrimidine sulfide derivatives containing a dithioacetal and strobilurin moiety were designed and synthesized. Their antiviral activities against tomato chlorosis virus (ToCV) were investigated through the tomato chlorosis virus coat protein (ToCVCP)-oriented screening method. Microscale thermophoresis was used to study the interaction between the compound and the ToCVCP. Compounds B13 and B23 interacted better with ToCVCP than the other compounds and had dissociation constant (K d) values of 0.09 and 0.06 μM, respectively. These values were lower than those of the control agents, ningnanmycin (0.19 μM) and ribavirin (6.54 μM), which indicated that the compounds had a strong binding effect with ToCVCP. Quantitative real-time polymerase chain reaction was used to evaluate the role of compounds B13 and B23 in the gene regulation of ToCVCP. Both compounds significantly reduced the expression level of the ToCVCP gene in Nicotiana benthamiana with reduction values of 88 and 83%, which were better than those of ningnanmycin (65%) and lead compound C14 (73%). Pyrimidine sulfide containing a dithioacetal and strobilurin moiety is significant in the research and development of novel anti-ToCV agents.

Tobacco mosaic virus (TMV) has caused huge economic losses to tobacco, pepper, cucumber, and ornamental crops all over the world. However, few effective antiviral agents were developed and applied to control such plant disease. It is challenging to find an anti-TMV agent which is highly effective, less toxic, and environmentally friendly. In this work, a series of ferulic acid ester-containing sulfonamide moieties were designed and synthesized, and the antiviral activities of these compounds against TMV were evaluated. The anti-TMV biological activity test showed that the target compounds showed excellent anti-TMV activity in vitro and in vivo . In particular, compound 2 has excellent anti-TMV activity at 500 μg/mL, which is higher than that of the control drug ribavirin. The preliminary mechanism research results showed that compound 2 can obviously destroy the morphology of the virions to show excellent activity. The results show that the ferulic acid ester-containing sulfonamide moiety deserves further research and development.

A number of novel chromone derivatives containing sulfonamide moieties were designed and synthesized, and the activity of compounds against tomato chlorosis virus (ToCV) was assessed using the ToCVCP-oriented screening method. Comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) models were established based on the dissociation constant (K d) values of the target compounds, and compound 35 was designed and synthesized with the aid of CoMFA and CoMSIA models. The study of affinity interaction indicated that compound 35 exhibited excellent affinity with ToCVCP with a K d value of 0.11 μM, which was better than that of the positive control agents xiangcaoliusuobingmi (0.44 μM) and ningnanmycin (0.79 μM). In addition, the in vivo inhibitory effect of compound 35 on the ToCVCP gene was evaluated by the quantitative real-time polymerase chain reaction. ToCVCP gene expression levels of the compound 35 treatment group were reduced by 67.2%, which was better than that of the positive control agent ningnanmycin (59.5%). Therefore, compound 35 can be used as a potential anti-ToCV drug in the future.

A rare Pb9 cluster-based organic framework constructed from a flexible cyclotriphosphazene-functionalized hexacarboxylate exhibits selective adsorption separation of C2 hydrocarbons and CO2 from CH4 under ambient conditions.