Objective： A series of 2-benzylideneaminonaphthothiazoles were designed and synthesized incorporating the lipophilic naphthalene ring to render them more capable of penetrating various biomembranes. Methods： Schiff ...Objective： A series of 2-benzylideneaminonaphthothiazoles were designed and synthesized incorporating the lipophilic naphthalene ring to render them more capable of penetrating various biomembranes. Methods： Schiff bases were synthesized by the reaction of naphtha[1,2-d]thiazol-2-amine with various substituted aromatic aldehydes. 2-（2＇-Hydroxy）ben- zylideneaminonaphthothiazole was converted to its Co（Ⅱ）, Ni（Ⅱ） and Cu（Ⅱ） metal complexes upon treatment with metal salts in ethanol. All the compounds were evaluated for their antibacterial activities by paper disc diffusion method with Gram positive Staphylococcus aureus and Staphylococcus epidermidis and Gram negative Escherichia coli and Pseudomonas aeruginosa bacteria. The minimum inhibitory concentrations of all the Schiff bases and metal complexes were determined by agar streak dilution method. Results： All the compounds moderately inhibited the growth of Cram positive and Gram negative bacteria. In the present study among all Schiff bases 2-（2＇-hydroxy）benzylideneaminonaphthothiazole showed maximum inhibitory activity and among metal complexes Cu（Ⅱ） metal complex was found to be most potent. Conclusion： The results obtained validate the hypothesis that Schiff bases having substitution with halogens, hydroxyl group and nitro group at phenyl ring are required for the antibacterial activity while methoxy group at different positions in the aromatic ring has minimal role in the inhibitory activity. The results also indicated that the metal complexes are better antibacterial agents as compared to the Schiff bases.展开更多
A series of alditol derivatives were designed and synthesized with relatively high yield. On the basis of reaction between sorbitol and a series of substituted benzaldehyde in the presence of an acid catalyst, a serie...A series of alditol derivatives were designed and synthesized with relatively high yield. On the basis of reaction between sorbitol and a series of substituted benzaldehyde in the presence of an acid catalyst, a series of acetal derivatives were synthesized through free hydroxyl esterification. D-sorbitol acetal amido derivatives were prepared by reduction of nitryl and acylation of amino. D-sorbitol acetal carboxyl esterification derivatives were prepared through esterification and hydrolysis. By high performance liquid chromatography-mass spectra (HPLC-MS) and 1H nuclear magnetic resonance spectra (1H-NMR), 36 compounds prepared were identified. Among these derivatives prepared, 26 compounds have not been reported in the previous literatures.展开更多
The title compound N-benzyl-1-ferrocenyl benzalimine, C24H21FeN, has been syn- thesized by a new method with molecular sieves (4 ? as catalyst, and its structure was determined by single-crystal X-ray diffraction. The...The title compound N-benzyl-1-ferrocenyl benzalimine, C24H21FeN, has been syn- thesized by a new method with molecular sieves (4 ? as catalyst, and its structure was determined by single-crystal X-ray diffraction. The crystal belongs to monoclinic, space group P21/c with a = 8.2298(16), b = 11.675(2), c = 19.556(4) ? b = 91.20(3)o, V = 1878.6(6) 3, Z = 4, Mr = 379.27, Dc = 1.341g/cm3, F(000) = 792, m = 0.809 mm-1, the final R = 0.0363 and wR = 0.0765 for 2809 observed reflections (I > 2s(I)). In the title compound, the Fe(1) atom is almost located at the center of the two cyclopentadienyl rings, with the Fe(1)Cp(1) and Fe(1)Cp(2) distances of 1.644(9) and 1.649(8) ? respectively. The two cyclopentadienyl rings are nearly parallel, and the dihedral angle between the ?5(C5H4) and ?5(C5H5) rings is 0.97(12)o. The C(11)=N unit is conjugated with the ?5(C5H4) ring which forms a dihedral angle of 101.3(2)o with the adjacent phenyl ring.展开更多
Two tri(2-chlorobenzyl)tin(IV) complexes with dithiocarbamate ligands (2-Cl- C6H4CH2)3SnS2CN(C5H10) 1 and (2-Cl-C6H4CH2)3SnS2CN(C4H9N) 2 have been synthesized by the reaction of tri(2-chlorobenzyl)tin(IV) chloride wit...Two tri(2-chlorobenzyl)tin(IV) complexes with dithiocarbamate ligands (2-Cl- C6H4CH2)3SnS2CN(C5H10) 1 and (2-Cl-C6H4CH2)3SnS2CN(C4H9N) 2 have been synthesized by the reaction of tri(2-chlorobenzyl)tin(IV) chloride with dithiocarbamates and characterized by elemental analysis, IR and 1H NMR. The crystal structures were determined by X-ray single-crystal diffraction. The crystal of complex 1 belongs to triclinic, space group P with a = 9.121(5), b = 10.788(6), c = 15.549(8) ? a = 77.812(6), b = 88.279(8), g = 72.023(6)o, Z = 2, V = 1421.5(13) ?, Dc = 1.532 g/cm3, ?= 1.344 mm-1, F(000) = 660, R = 0.0382 and wR = 0.0984; and that of complex 2 is of monoclinic, space group P21/n with a = 13.892(10), b = 2.1274(8), c = 2.0553(15) ? b = 107.145(11)o, Z = 4, V = 2726(3) ?, Dc = 1.600 g/cm3, ?= 1.403 mm-1, F(000) = 1320, R = 0.0361 and wR = 0.0826. Their structures show a distorted trigonal bipyramidal configuration with five- coordination for the central tin atoms.展开更多
文摘Objective： A series of 2-benzylideneaminonaphthothiazoles were designed and synthesized incorporating the lipophilic naphthalene ring to render them more capable of penetrating various biomembranes. Methods： Schiff bases were synthesized by the reaction of naphtha[1,2-d]thiazol-2-amine with various substituted aromatic aldehydes. 2-（2＇-Hydroxy）ben- zylideneaminonaphthothiazole was converted to its Co（Ⅱ）, Ni（Ⅱ） and Cu（Ⅱ） metal complexes upon treatment with metal salts in ethanol. All the compounds were evaluated for their antibacterial activities by paper disc diffusion method with Gram positive Staphylococcus aureus and Staphylococcus epidermidis and Gram negative Escherichia coli and Pseudomonas aeruginosa bacteria. The minimum inhibitory concentrations of all the Schiff bases and metal complexes were determined by agar streak dilution method. Results： All the compounds moderately inhibited the growth of Cram positive and Gram negative bacteria. In the present study among all Schiff bases 2-（2＇-hydroxy）benzylideneaminonaphthothiazole showed maximum inhibitory activity and among metal complexes Cu（Ⅱ） metal complex was found to be most potent. Conclusion： The results obtained validate the hypothesis that Schiff bases having substitution with halogens, hydroxyl group and nitro group at phenyl ring are required for the antibacterial activity while methoxy group at different positions in the aromatic ring has minimal role in the inhibitory activity. The results also indicated that the metal complexes are better antibacterial agents as compared to the Schiff bases.
基金National Natural Science Foundation of China (No 20306022)
文摘A series of alditol derivatives were designed and synthesized with relatively high yield. On the basis of reaction between sorbitol and a series of substituted benzaldehyde in the presence of an acid catalyst, a series of acetal derivatives were synthesized through free hydroxyl esterification. D-sorbitol acetal amido derivatives were prepared by reduction of nitryl and acylation of amino. D-sorbitol acetal carboxyl esterification derivatives were prepared through esterification and hydrolysis. By high performance liquid chromatography-mass spectra (HPLC-MS) and 1H nuclear magnetic resonance spectra (1H-NMR), 36 compounds prepared were identified. Among these derivatives prepared, 26 compounds have not been reported in the previous literatures.
基金This work was supported by the Fundamental Research Fund of Beijing Institute of Technology
文摘The title compound N-benzyl-1-ferrocenyl benzalimine, C24H21FeN, has been syn- thesized by a new method with molecular sieves (4 ? as catalyst, and its structure was determined by single-crystal X-ray diffraction. The crystal belongs to monoclinic, space group P21/c with a = 8.2298(16), b = 11.675(2), c = 19.556(4) ? b = 91.20(3)o, V = 1878.6(6) 3, Z = 4, Mr = 379.27, Dc = 1.341g/cm3, F(000) = 792, m = 0.809 mm-1, the final R = 0.0363 and wR = 0.0765 for 2809 observed reflections (I > 2s(I)). In the title compound, the Fe(1) atom is almost located at the center of the two cyclopentadienyl rings, with the Fe(1)Cp(1) and Fe(1)Cp(2) distances of 1.644(9) and 1.649(8) ? respectively. The two cyclopentadienyl rings are nearly parallel, and the dihedral angle between the ?5(C5H4) and ?5(C5H5) rings is 0.97(12)o. The C(11)=N unit is conjugated with the ?5(C5H4) ring which forms a dihedral angle of 101.3(2)o with the adjacent phenyl ring.
基金The National Natural Science Foundation of China (No.20271025) and the Natural Science Foundation of Shandong Province (No. L2003B01)
文摘Two tri(2-chlorobenzyl)tin(IV) complexes with dithiocarbamate ligands (2-Cl- C6H4CH2)3SnS2CN(C5H10) 1 and (2-Cl-C6H4CH2)3SnS2CN(C4H9N) 2 have been synthesized by the reaction of tri(2-chlorobenzyl)tin(IV) chloride with dithiocarbamates and characterized by elemental analysis, IR and 1H NMR. The crystal structures were determined by X-ray single-crystal diffraction. The crystal of complex 1 belongs to triclinic, space group P with a = 9.121(5), b = 10.788(6), c = 15.549(8) ? a = 77.812(6), b = 88.279(8), g = 72.023(6)o, Z = 2, V = 1421.5(13) ?, Dc = 1.532 g/cm3, ?= 1.344 mm-1, F(000) = 660, R = 0.0382 and wR = 0.0984; and that of complex 2 is of monoclinic, space group P21/n with a = 13.892(10), b = 2.1274(8), c = 2.0553(15) ? b = 107.145(11)o, Z = 4, V = 2726(3) ?, Dc = 1.600 g/cm3, ?= 1.403 mm-1, F(000) = 1320, R = 0.0361 and wR = 0.0826. Their structures show a distorted trigonal bipyramidal configuration with five- coordination for the central tin atoms.
