the beta0diketone derivatives of nitroimidazole were synthesized from the reaction of magnesium salt of beta-ketoaccids 3 with imidazolide 4. the raction of beta-diketones with hydroxylamine hydrochloride afforded either the isoxazoles or the 5-hydroxyl-2-isoxazolines.

The reaction of 3-allyl-1,5-dimethyl-1,5-benzodiazepine-2,4-dione and benzaldoxime leads to the title compound, C(21)H(21)N(3)O(3). The mol-ecular structure is built up from two fused six- and seven-membered rings linked to a chain including a five- and six-membered ring (isoxazoline and phen-yl) via a methyl-ene group. The seven-membered ring displays a boat conformation. The dihedral angle be...

In the title compound, C(10)H(13)NO(2)S, the thio-phene and isoxazoline rings are almost coplanar, the dihedral angle between their least-squares planes being 2.08 (1)°. The O-H atoms of the methyl hy-droxy group and the N atom of the isoxazole ring are orientated in the same direction to allow for the formation of inter-molecular O-H⋯N hydrogen bonds that lead to a supra-molecular chain along ...

Benzonitrile oxide (la) reach with 1,1,2,2,3,3-hexamethyl-4,5-bis(methylene)cyclopen~e (5) to give a mixture of the 1,3-dipolar cycloaddition product 8 and the oxime 9. This reaction is 26 times slower than the corresponding reaction of la with 1,2-bis(methylene)cyclopentane (15), which exclusively yields the 2-isoxazoline 19. With the assumption that the oxime 9 is generated by a stepwise proc...

A new isoxazoline compound (5-(2,6-difluorobenzyl)oxymethyl-5-methyl-3(3-methylthiophen-2-yl)-1,2-isoxazoline; code name, EK-5229) was reported to have safety in rice and control barnyardgrass (Echinochloa crus-galli), but its mode of action was unknown. The compound did not inhibit germination of sensitive grasses, but it inhibited further growth. The symptom was primarily stunting and discolo...

There is a need for robust in vitro models to sensitively capture skeletal muscle adverse toxicities early in the research and development of novel xenobiotics. To this end, an in vitro rat skeletal muscle model (L6) was used to study the translation of transcriptomics data generated from an in vivo rat model. Novel sulfonyl isoxazoline herbicides were associated with skeletal muscle toxicity i...

The current synthesis of racemic purine and pyrimidine isoxazoline-carbocyclic nucleosides is reported, detailing the key-steps for standard and reliable preparations. Improved yields were obtained by the proper tuning of the single synthetic steps, opening the way for the preparation of a variety of novel compounds. Some of the obtained compounds were also evaluated against a wide variety of D...