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C18H20F12N4P2, monoclinic, P21/n (no. 14), a = 8.3185(9) Å, b = 21.883(2) Å, c = 13.4345(15) Å, β = 103.4730(10)°, V = 2378.3(5) Å3, Z = 4, Rgt(F) = 0.0470, wRref(F2) = 0.1305, T = 296(2) K. [ABSTRACT FROM AUTHOR]

• 36 novel pyrazolyl amide compounds with a pyridine ring structure were designed and synthesized. The structures of the compounds were confirmed. • The compound 2i was confirmed by single-crystal X-ray diffraction. • The fungicidal effects of the newly designed compounds on four plant pathogenic fungi were determined by the mycelial growth rate method. • Compound 1g has a good inhibitory effect on the growth of a variety of plant pathogenic fungi. • The molecular docking studies of the representative compounds were performed. With the help of active substructure splicing strategy, 36 novel pyridine ring pyrazolamide derivatives were designed and synthesized. The structures of those compounds were confirmed and characterized by 1H NMR, 13C NMR, FT-IR, and HRMS. The compound 2i was identified by X-ray crystal diffraction. The fungicidal effects of the pyrazolamide derivates against four plant pathogenic fungi, Colletotrichum gloeosporioides, Fusarium oxysporum, Sphaeropsis sapinea and Fusarium moniliforme , was determined by the mycelial growth rate. The results showed that the designed compounds had certain antifungal activity at the concentration of 200 mg/L. Compared with the positive control carbendazim, compounds 1e , 1g and 1h exhibited stronger antifungal activity on Sphaeropsis sapinea and Fusarium moniliforme. The antifungal activity of compound 1a- 1s (R1 = H) was better than that of compound 2a-2p (R1 = CH 3). Compounds 1d, 1e , 1g, 1h, 1i , 2g and 2i showed good antifungal activity, and the introduction of halogen groups (except F) on benzene ring may have an important effect on biological activity. Compound 1g had a good inhibitory effect on the growth of a variety of plant pathogenic fungi. Molecular docking revealed that the -CH 3 group at R1 position would reduce the binding affinity between these compounds and receptor, which would reduce the antifungal activity of the compound. Compound 1g is promising to become the lead compound of pesticide in the future, which is worthy of further study. [Display omitted] [ABSTRACT FROM AUTHOR]

Rice (Oryza sativa L.), a major staple crop worldwide, has limited levels of the essential amino acid lysine. We previously produced engineered rice with increased lysine content by expressing bacterial aspartate kinase and dihydrodipicolinate synthase and inhibiting rice lysine ketoglutarate reductase/saccharopine dehydrogenase activity. However, the grain quality, field performance, and integration patterns of the transgenes in these lysine-enriched lines remain unclear. In the present study, we selected several elite transgenic lines with endosperm-specific or constitutive regulation of the above key enzymes but lacking the selectable marker gene. All target transgenes were integrated into the intragenic region in the rice genome. Two pyramid transgenic lines (High Free Lysine; HFL1 and HFL2) with free lysine levels in seeds up to 25-fold that of wild type were obtained via a combination of the above two transgenic events. We observed a dramatic increase in total free amino acids and a slight increase in total protein content in both pyramid lines. Moreover, the general physicochemical properties were improved in pyramid transgenic rice, but the starch composition was not affected. Field trials indicated that the growth of HFL transgenic rice was normal, except for a slight difference in plant height and grain colour. Taken together, these findings will be useful for the potential commercialization of high-lysine transgenic rice. [ABSTRACT FROM AUTHOR]

C15H20ClN3O, monoclinic, C2/ c (no. 15), a = 19.300(2) Å, b = 10.8262(11) Å, c = 15.4282(16) Å, β = 100.457(4)°, V = 3170.0(6) Å3, Z = 8, Rgt (F) = 0.0409, wRref (F2) = 0.1150, T = 296(2) K. [ABSTRACT FROM AUTHOR]

C14H24F12N4P2, triclinic, P1̅ (no. 2), a = 8.8173(12) Å, b = 8.8845(12) Å, c = 9.1494(12) Å, α = 62.2060(10)°, β = 64.2980(10)°, γ = 89.661(2)°, V = 553.72(13) Å3, Z = 1, Rgt( F) = 0.0746, wRref( F2) = 0.2038, T = 296 K. [ABSTRACT FROM AUTHOR]