A series of novel substituted thiazide/thiazole compounds were designed by splicing active groups and bioisosterism. The title compounds were synthesized via the cyclization, acylation, and carbamylation. All the compounds were characterized by IR, 1H‐NMR, 13C‐NMR, and HRMS. The single crystal of compound 3f was determined by X‐ray crystallography. The biological activity tests indicated that all the compounds showed potential safener activity to the herbicide chlorsulfuron, in which compound 3e showed almost the same level as the commercialized safener AD‐67. The molecular docking results were in good agreement with the bioassay results, which demonstrated that compound 3e might compete with chlorsulfuron in the acetolactate synthase active site, causing the herbicide ineffective in maize.
TF5. -Eight new metabolites, including new sesquiterpenoids (I), a new backbone sesquiterpene rearranged from guaiane, two disecoguaianes (II), two new dihydroisocoumarins (IV), and one new tetralone (III) are isolated together with ten known compounds. None of the new compounds shows antimicrobial activities. -(LU, C.-H.; LIU, S.-S.; WANG, J.-Y.; WANG, M.-Z.; SHEN*, Y.-M.; Helv. Chim. Acta 97 (2014) 3, 334-344, http://dx.
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