A variety of new (3-Z)-3-((alkyl/aryl)aminomethylene)-4-(2-hydroxyphenyl)-1,3-dihydro-2H-1,5-benzodiazepin-2-ones were synthesized via addition of primary amines on the benzopyrano[4,3-c]-1H-1,5-benzodizepin-2one. High yields with excellent diastereoselectivity were obtained. The structure of cis-β-enamino-1,5benzodiazepine derivatives was characterized by 1D and 2D NMR and confirmed by an X-Ray diffraction analysis. All prepared compounds were evaluated for their in vitro antibacterial activities and promising results were given.
Novel N-substituted pyrrolo [3,4-b]quinoline-1,3-diones have been prepared via a highly chemoselective palladium-catalyzed carbonylative imidazation-cyclization reaction in a one-pot synthetic approach. This methodology, which has been applied for the first time to access such original scaffolds through two different protocols involving 3-bromo-2-iodoquinoline, as a typical partner, primary amines, and atmospheric or high carbon monoxide pressure (20 bar), has shown an excellent tolerance for many functional groups. The use of bidentate ligands such as XantPhos and dppp, either under atmospheric or high-pressure conditions, provides a wide range of carbonylated compounds in good to excellent yields (up to 82 %). Furthermore, some new quinoline-2,3-dicarboxamides have been isolated as side products in very low yields and have been fully characterized. The solid state structures of three of the synthesized acridinimides have been unequivocally established by single-crystal XRD analysis.
Novel 1,2,3-triazolo-linked-1,5-benzodiazepinones were designed and synthesized via a Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction (CuAAC). The chemical structures of these compounds were confirmed by 1H NMR, 13C NMR, HMBC, HRMS, and elemental analysis. The compounds were screened for their in vitro antibacterial and antifungal activities. Several compounds exhibited good to moderate activities compared to those of established standard drugs. Furthermore, the binding interactions of these active analogs were confirmed through molecular docking.
Both theoretical and experimental study of a three-components one-pot cycloaddition reaction involving unstabilized azomethine ylides and unsymmetrical exocyclic dienones featuring a tetralone core was performed. Two new families of highly...
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.