Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice

A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. It was found that aromatic groups coupled to Mannich phenols and the introduction of imidazole to the ortho position of phenols would dramatically enhance reactivation efficiency. Moreover, the in vivo experiment was conducted, and the results demonstrated that Mannich phenol L10R1 (30 mg/kg, ip) could afford 100% 48 h survival for mice of 2*LD50 sarin exposure, which is promising for the development of non-oxime reactivators with central efficiency

Inhibitory Mechanisms of <i>trans</i>-2-Hexenal on the Growth of <i>Geotrichum citri</i>-<i>aurantii</i>

Geotrichum citri-aurantii (G. citri-aurantii) is one of the most important postharvest pathogens leading to a postharvest loss of citrus by causing sour rot. In this study, the antifungal activity of trans-2-hexenal, a natural component of essential oil, against G. citri-aurantii was evaluated. Trans-2-hexenal treatment inhibited the mycelia growth of G. citri-aurantii with a minimum inhibitory concentration and minimum fungicidal concentration of trans-2-hexenal at 0.50 and 1.00 μL/mL, respectively. Moreover, trans-2-hexenal efficiently reduced the incidence of sour rot of Satsuma fruit inoculated with G. citri-aurantii. Ultrastructural observations and Fourier transform infrared (FT−IR) results showed that trans-2-hexenal treatment affected the cell wall and cell membrane instructions of G. citri-aurantii. The content of β-1,3-glucan was significantly decreased after trans-2-hexenal treatment, but the cell wall permeability was not changed. The decrease in lipid and ergosterol contents might be responsible for this antifungal activity. Several important genes, FKS1, ERG1, ERG7, and ERG11, showed decreasing expression levels after trans-2-hexenal treatment. Molecule-docking results also indicated that trans-2-hexenal could join with the protein of FKS1, ERG1, ERG7, and ERG11 to impact enzyme activities. These results demonstrated that trans-2-hexenal is a promising fungicide for controlling sour rot of harvested citrus fruit by damaging the membrane integrity of G. citri-aurantii.</i

Concise and Gram-Scale Total Synthesis of Lansiumamides A and B and Alatamide

The total synthesis of potent anti-obesity lansiumamide B was accomplished in four steps using commercially available materials. The synthetic strategy, featured with copper-catalyzed Buchwald coupling, is concise, convergent, practical and can be carried out on a one-gram scale. This approach could give either Z- or E-configured enamide moiety in natural products with absolute stereocontrol and was applied in the total synthesis of natural products