An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydr...An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first time.The catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains.The outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against E.coil.Whereas,compound 6f and 6h exhibited excellent activity against P.aeurginosa,and compound 6c,and 6e displayed again excellent activity against Staphylococcus aureus whereas compound 7o shows excellent activity against S.aureus and B.subtilis when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.展开更多
Two new crystalline materials[Cu_(3)(μ_(2)-H_(3)bis-tris)_(2)(μ_(2)-Hhpa)_(2)]·H_(2)O(1)and[Cu_(3)(μ_(2)-H_(2)tea)_(2)(μ_(2)-hpa)-(μ_(3)-hpa)]_(n)(2)bearing distinct tricopper(Ⅱ)cores were easily generated ...Two new crystalline materials[Cu_(3)(μ_(2)-H_(3)bis-tris)_(2)(μ_(2)-Hhpa)_(2)]·H_(2)O(1)and[Cu_(3)(μ_(2)-H_(2)tea)_(2)(μ_(2)-hpa)-(μ_(3)-hpa)]_(n)(2)bearing distinct tricopper(Ⅱ)cores were easily generated by the aqueous medium selfassembly method from copper(Ⅱ)nitrate,bis(2-hydroxyethyl)amino-tris(hydroxymethyl)methane(H_(5)bistris)or triethanolamine(H_(3)tea)aminoalcohol biobuffers and homophthalic acid(H_(2)hpa).The obtained products were characterised by IR,UV-vis and EPR spectroscopy,ESI-MS(±),thermogravimetric,elemental and single crystal X-ray diffraction analysis.Apart from possessing different dimensionality,the crystal structures of the discrete 0D trimer 1 and the zigzag 1D coordination polymer 2 show distinct symmetric[Cu_(3)(μ-O)_(4)(μ-COO)_(2)]and asymmetric[Cu_(3)(μ-O)_(3)(μ-COO)_(2)]tricopper(Ⅱ)cores,respectively.An intense pattern of intermolecular O-H…O hydrogen bonds provides a 0D→3D(1)or 1D→2D(2)extension of the structures into intricate topologically unique H-bonded nets.After additional simplification,these were classified as a uninodal 6-connected 3D framework with the snk topology in 1 and a binodal 3,5-connected 2D layer with the 3,5L50 topology in 2.Variable-temperature magnetic susceptibility studies indicate a predominant ferromagnetic coupling[J=39.1(1)and 29.5(1)cm^(−1)for 1 and 2,respectively]within the mixed-bridged tricopper(Ⅱ)cores.Both compounds 1 and 2 were also applied as rather efficient bio-inspired pre-catalysts for the mild homogeneous oxidation,by aqueous H_(2)O_(2)at 50℃in acidic MeCN-H_(2)O medium,of cyclic(cyclopentane,cyclohexane,cycloheptane and cyclooctane)and linear(n-pentane,n-hexane,n-heptane and n-octane)alkanes to the corresponding alcohols and ketones with overall yields up to 26%based on the alkane.The effects of different reaction parameters(type of pre-catalyst and acid promoter,reaction time and substrate scope)and various selectivity features were investigated and discussed,supporting a free-radical mechanism in the present alkane oxidations.展开更多
基金supported by Special Assistance Programme SAP,University Grants Commission,New Delhi,India
文摘An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first time.The catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial strains.The outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against E.coil.Whereas,compound 6f and 6h exhibited excellent activity against P.aeurginosa,and compound 6c,and 6e displayed again excellent activity against Staphylococcus aureus whereas compound 7o shows excellent activity against S.aureus and B.subtilis when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.
基金supported by the Foundation for Science and Technology(FCT)(projects PTDC/QUI-QUI/121526/2010,RECI/QEQ-QIN/0189/2012,PEst-OE/QUI/UI0100/2013,IF/01395/2013 and SFRH/BPD/78854/2011),Portugal.
文摘Two new crystalline materials[Cu_(3)(μ_(2)-H_(3)bis-tris)_(2)(μ_(2)-Hhpa)_(2)]·H_(2)O(1)and[Cu_(3)(μ_(2)-H_(2)tea)_(2)(μ_(2)-hpa)-(μ_(3)-hpa)]_(n)(2)bearing distinct tricopper(Ⅱ)cores were easily generated by the aqueous medium selfassembly method from copper(Ⅱ)nitrate,bis(2-hydroxyethyl)amino-tris(hydroxymethyl)methane(H_(5)bistris)or triethanolamine(H_(3)tea)aminoalcohol biobuffers and homophthalic acid(H_(2)hpa).The obtained products were characterised by IR,UV-vis and EPR spectroscopy,ESI-MS(±),thermogravimetric,elemental and single crystal X-ray diffraction analysis.Apart from possessing different dimensionality,the crystal structures of the discrete 0D trimer 1 and the zigzag 1D coordination polymer 2 show distinct symmetric[Cu_(3)(μ-O)_(4)(μ-COO)_(2)]and asymmetric[Cu_(3)(μ-O)_(3)(μ-COO)_(2)]tricopper(Ⅱ)cores,respectively.An intense pattern of intermolecular O-H…O hydrogen bonds provides a 0D→3D(1)or 1D→2D(2)extension of the structures into intricate topologically unique H-bonded nets.After additional simplification,these were classified as a uninodal 6-connected 3D framework with the snk topology in 1 and a binodal 3,5-connected 2D layer with the 3,5L50 topology in 2.Variable-temperature magnetic susceptibility studies indicate a predominant ferromagnetic coupling[J=39.1(1)and 29.5(1)cm^(−1)for 1 and 2,respectively]within the mixed-bridged tricopper(Ⅱ)cores.Both compounds 1 and 2 were also applied as rather efficient bio-inspired pre-catalysts for the mild homogeneous oxidation,by aqueous H_(2)O_(2)at 50℃in acidic MeCN-H_(2)O medium,of cyclic(cyclopentane,cyclohexane,cycloheptane and cyclooctane)and linear(n-pentane,n-hexane,n-heptane and n-octane)alkanes to the corresponding alcohols and ketones with overall yields up to 26%based on the alkane.The effects of different reaction parameters(type of pre-catalyst and acid promoter,reaction time and substrate scope)and various selectivity features were investigated and discussed,supporting a free-radical mechanism in the present alkane oxidations.
