3D magnetic flower-spherical Fe2O3-NiO derived from NiFe-layered double hydroxides for the efficient removal of Bensulfuron methyl: Morphological control and bimetallic synergy.

Three-dimensional (3D) magnetic flower-spherical Fe2O3-NiO derived from NiFe-layered double hydroxides (NiFe-LDHs) was fabricated through urea hydrothermal and calcination methods. The as-prepared materials were applied to activate PMS to degrade one of herbicide named Bensulfuron methyl (BSM). Fe2O3-NiO-1 demonstrated the highest catalytic activity and the lowest ions leaching by comparing the performance of LDHs and derivative bimetallic oxide synthesized by co-precipitation method, urea hydrothermal method and direct calcination method. Based on the results of SEM, BET and CV, the high catalytic activity of Fe2O3-NiO-1 originated from 3D morphology, lager specific area and pore size and faster electron transfer capability. The factors influencing the degradation performance were investigated and 0.1 g·L-1 Fe2O3-NiO could effectively activate PMS (1 mmol·L-1) to completely remove 10 mg·L-1 BSM within 30 min at pH 7.0. In Fe2O3-NiO/PMS system, OH, SO4- and 1O2 were produced and contributed to the BSM removal according to the results of EPR and quenching experiments. In order to expand its application range, Fe2O3-NiO/PMS system was used to degrade aniline (AN), sulfamethoxazole (SMZ), phenacetin (PNT), bisphenol A (BPA) and 2,4,6-triclofen (2,4,6-TCP) and the results showed the degradation efficiency could reach 90 % or more. Additionally, the application of catalysts in different actual water samples and the ability of reuse were tested. Based on the strategies of bimetallic synergy and morphology control, Fe-based bimetallic oxides with 3D morphology were developed in this study, which could effectively enhance the catalytic activity and inhibit the dissolution of metal ions, providing the design ideas for the construction of efficient catalysts and the removal of complex organic pollutants.

Streptochlorin analogues as potential antifungal agents: Design, synthesis, antifungal activity and molecular docking study.

Streptochlorin is a small molecule of indole alkaloid isolated from marine Streptomyces sp., it is a promising lead compound due to its potent bioactivity in preventing many phytopathogens in our previous study, but further structural modifications are required to improve its antifungal activity. Our work in this paper focused on the replacement of oxazole ring in streptochlorin with the imidazole ring, to discover novel analogues. Based on this design strategy, three series of streptochlorin analogues were efficiently synthesized through sequential Vilsmeier-Haack reaction, Van Leusen imidazole synthesis and halogenation reaction. Some of the analogues displayed excellent activity in the primary assays, and this is highlighted by compounds 4g and 4i, the growth inhibition against Alternaria Leaf Spot and Rhizoctorzia solani under 50 µg/mL are 97.5% and 90.3%, respectively, even more active than those of streptochlorin, pimprinine and Osthole. Molecular docking models indicated that streptochlorin binds with Thermus thermophiles Leucyl-tRNA Synthetase in a similar mode to AN2690, offering a perspective on the mode of action study for antifungal activities of streptochlorin derivatives. Further study is still ongoing with the aim of discovering synthetic analogues, with improved antifungal activity and clear mode of action.

Diversity-oriented synthesis and antifungal activities of novel pimprinine derivative bearing a 1,3,4-oxadiazole-5-thioether moiety.

Based on the strategy of diversity-oriented synthesis and the structures of natural product pimprinine and streptochlorin, two series of novel pimprinine derivatives containing 1,3,4-oxadiazole-5-thioether moieties were efficiently synthesized under the optimized reaction conditions. Biological assays conducted at Syngenta showed the designed derivatives displayed an altered pattern of biological activity, of which 5h was identified as the most promising compound with strong activity against Pythium dissimile and also a broad antifungal spectrum in primary screening. Further structural optimization of pimprinine and streptochlorin derivatives is well under way, aiming to discover synthetic analogues with improved antifungal activity. Two series of novel pimprinine derivatives containing 1,3,4-oxadiazole-5-thioether moieties were efficiently synthesized through diversity-oriented synthesis strategy under the optimized conditions. Biological assays showed the designed derivatives exhibited potential activity.