The present study observed the action of 1H-indole-2, 3-dione (isatin) on Bax protein expression in the substantia nigra of a Parkinson's disease animal model. Parkinson's disease-like behaviors were induced in C5...The present study observed the action of 1H-indole-2, 3-dione (isatin) on Bax protein expression in the substantia nigra of a Parkinson's disease animal model. Parkinson's disease-like behaviors were induced in C57BL/6J mice treated with 1-methyl-4-phenyl-1,2, 3, 6-tetrahydropyridine (MPTP) Bax protein expression was significantly reduced in isatin (100, 200 mg/kg)-pretreated mice. Results demonstrate that isatin plays a neuroprotective role in mice treated with MPTP by down-regulating Bax protein expression.展开更多
A series of novel moxifloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity, compared to the parent moxifloxacin, was designed, synthesized and characterized by 1H NMR, MS and...A series of novel moxifloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity, compared to the parent moxifloxacin, was designed, synthesized and characterized by 1H NMR, MS and HRMS. These derivatives were initially evaluated for their in vitro antimycobacterial activity against M. smegmatis CMCC 93202. Compounds 3a―3f, 5a, 5f and 5j were chosen for the further evaluation of their in vitro activity against Mycobacterium tuberculosis(MTB) H37Rv ATCC 27294 and MDR-MTB 09710. All the target com pounds[minimum inhibitory concentration(MIC): 0.39―〉16 μg/mL] were far more active than rifampin(MIC: 2.0―〉256 μg/mL), but less active than moxifloxacin(MIC: 0.1―1.0 μg/mL) against the three tested strains. The most active compounds 3a and 3c were found to be 2―64 fold more potent than isoniazid and rifampin against M. smegmatis CMCC 93202, 2 fold more potent than rifampin against MTB H37Rv ATCC 27294, and 16―〉64 fold more potent than ethambutol, isoniazid and rifampin against MDR-MTB 09710.展开更多
Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecule...Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecules due to the restricted structural features to serve in the laser desorption/ionization mechanism with a problem of background signals appearing in the low mass region. This paper describes the application of Schiff base derivatives of acylhydrazide and isatin as alternate UV-LDI matrices for the analysis of peptides with significantly low background signals. Thirty one compounds have been successfully employed as matrices for the analysis of low molecular weight (LMW) peptides (α-Cyano-4-hydroxycinnamic acid (HCCA), a preferred choice for peptide analysis.展开更多
A new approach to synthesis of 6,7-dimethoxyisatin is reported. 2-nitro-3, 4- dimethoxy mandelonitrile in glacial acetic acid was treated with the solution of stannous chloride in hydrochloric acid to give 6, 7-dimet...A new approach to synthesis of 6,7-dimethoxyisatin is reported. 2-nitro-3, 4- dimethoxy mandelonitrile in glacial acetic acid was treated with the solution of stannous chloride in hydrochloric acid to give 6, 7-dimethoxyisatin in a high yield.展开更多
The title compounds(Z)-3-(2-(3-chloropyridin-2-yl)hydrazono)indolin-2-one(A) and 7-bromo-(Z)-3-((4-pyridinyl)carboxlichydrazono)-2-indolinone(B) have been synthesized and structurally determined by ele...The title compounds(Z)-3-(2-(3-chloropyridin-2-yl)hydrazono)indolin-2-one(A) and 7-bromo-(Z)-3-((4-pyridinyl)carboxlichydrazono)-2-indolinone(B) have been synthesized and structurally determined by elemental analysis and single-crystal X-ray diffraction studies.Compound A(C13H8ClN4O) belongs to the orthorhombic crystal system,space group Pca21 with a = 20.799(4),b = 4.9312(10),c = 11.764(2),V = 1206.6(4)3,Mr = 271.68,Dc = 1.496 g/cm3,μ = 0.313 mm-1,F(000) = 556,Z = 4,the final R = 0.0346 and wR = 0.0831 for 2683 observed reflections with I 2σ(I).Compound B(C14H9BrN4O2) belongs to the triclinic crystal system,space group P1 with a = 6.6834(13),b = 7.0727(14),c = 14.285(3),α = 95.56(3),β = 99.00(3),γ = 102.95(3)°,V = 643.8(2)3,Mr = 345.16,Dc = 1.780 g/cm3,μ = 3.203 mm-1,F(000) = 344,Z = 2,the final R = 0.0487 and wR = 0.1167 for 2334 observed reflections with I 2σ(I).The preliminary herbicidal bioassay reveals that compounds A and B have some inhibition both in vivo and in vitro against AHAS.展开更多
Two novel compounds 1-(4-fluorobenzyl)-4-chloro-(Z)-3-benzoylhydrazono-2-indolinone(1) and 1-(4-methoxybenzyl)-(Z)-3-benzoylhydrazono-2-indolinone(2) were synthesized and their crystal structures were dete...Two novel compounds 1-(4-fluorobenzyl)-4-chloro-(Z)-3-benzoylhydrazono-2-indolinone(1) and 1-(4-methoxybenzyl)-(Z)-3-benzoylhydrazono-2-indolinone(2) were synthesized and their crystal structures were determined by single-crystal X-ray diffraction.Compound 1(C22H15ClFN3O2) crystallized in the triclinic system,space group P1·with a=0.94198(19) nm,b=1.4339(3) nm,c=1.5018(3) nm,α=101.58(3)°,β=102.96(3)°,γ=102.73°,V=1.8602(6) nm3,Mr=407.82,Dc=1.456 g/cm3,μ=0.240 mm-1,F(000)=840,Z=4,R1=0.0442 and wR2=0.1064.Compound 2(C23H19N3O3) crystallized in the triclinic system,space group P1·with a=1.0022(2) nm,b=1.0192(2) nm,c=1.0461(2) nm,α=99.86(3)°,β=117.30(3)°,γ=94.13(3)°,V=0.9215(3) nm3,Mr=385.41,Dc=1.389 g/cm3,μ=0.094 mm-1,F(000)=404,Z=2,R1=0.0403 and wR2=0.1142.The preliminary herbicidal activities of the two compounds were also evaluated.展开更多
New dibutyltin(IV) complexes of Schiff base derived from 5-chloroindoline-2,3-dione, indoline- 2,3-dione with amino acids (tryptophan, alanine and valine) were synthesized and characterized by elemental analysis, IR, ...New dibutyltin(IV) complexes of Schiff base derived from 5-chloroindoline-2,3-dione, indoline- 2,3-dione with amino acids (tryptophan, alanine and valine) were synthesized and characterized by elemental analysis, IR, electronic spectra, conductance measurements, and biological activity. The analytical data showed that the Schiff base ligand acts as bidentate towards metal ions via the azomethine nitrogen and carboxylate oxygen by a stoichiometric reaction of M:L (1:2) to form metal complexes. NMR (1H, 13C and 119Sn) spectral data of the ligands and metal complex agree with proposed structures. The conductivity values between 14 - 27 ohm-1cm2mol-1 in DMF imply the presence of non-electrolyte species. 3D molecular modeling and analysis of bond lengths and bond angles have also been conducted for a representative compound, [Bu2Sn(L2)2], to substantiate the proposed structures. Antibacterial results indicate that the metal complexes are more active than the free ligands.展开更多
The effects of isatin (2,3-dioxo-indole) and isatin analogues (5-methylisatin, 6-hydroxyisatin, 7-ethylisatin, N-acety- lisatin) were tested on prostaglandin E2 (PGE2)-induced fever in mice and rats. Two modes of admi...The effects of isatin (2,3-dioxo-indole) and isatin analogues (5-methylisatin, 6-hydroxyisatin, 7-ethylisatin, N-acety- lisatin) were tested on prostaglandin E2 (PGE2)-induced fever in mice and rats. Two modes of administration were tested. Isatin or an analogue was injected simultaneously with PGE2 and the development of fever was tested, or the test compound was given 30 min following PGE2 administration and the effects on the already existing fever were measured, in mice and in rats. Isatin in a dose of 3.12 mg/kg ip was found to block the development of PGE2-induced fever in mice, while in a dose of 12.5 mg/kg ip it attenuated the existing fever. In rats isatin in a dose of 12.5 mg/kg ip blocked fever initiation, and at 25.0 mg/kg ip attenuated existing PGE2-induced fever. In mice, 5-methylisatin in a dose of 0.21 mg/kg ip blocked the initiation of fever, and at 6.72 mg/kg ip attenuated the existing fever. In rats in a dose of 3.36 mg/kg ip it blocked the development of fever, and at 13.44 mg/kg ip attenuated existing PGE2-induced fever. In mice 5,6-dimetylisatin in a dose of 0.02 mg/kg ip both blocked fever initiation and attenuated the existing fever in mice, in rats in a dose of 0.42 mg/kg ip it blocked the initiation of fever, and at 0.21 mg/kg ip attenuated the existing PGE2-induced fever. In mice 6-hydroxyisatin in a dose of 5.2 mg/kg blocked the development of fever, and at 10.4 mg/kg attenuated the existing fever. In rats in a dose of 10.40 mg/kg ip it blocked fever development and also attenuated the existing fever. In mice, 7-ethylisatin in a dose of 0.02 mg/kg ip both blocked fever initiation and also attenuated the existing fever. In rats, a dose of 0.11 mg/kg both blocked fever initiation and also attenuated the existing fever. In mice, N-acethylisatin in the dose of 0.005 mg/kg blocked fever initiation, while at 1.024 mg/kg it attenuated existing fever, in rats, in a dose of 0.096 mg/kg it blocked fever initiation, and at 0.384 mg/kg attenuated the existing fever. The results demonstrate that 7-ethyl- and N-acetylisatin are the most effective of these compounds both in blocking the development of PGE2-induced fever and also in attenuating existing the PGE 2-induced fever.展开更多
Schiff base ligand (HL) derived from 4-hexylaniline with isatin (1H-indole-2,3-dione) and its complexes with Cu(Ⅱ), Ni(Ⅱ) were prepared and characterized by analytical, spectroscopic (IR, UV-Vis, Mass) tec...Schiff base ligand (HL) derived from 4-hexylaniline with isatin (1H-indole-2,3-dione) and its complexes with Cu(Ⅱ), Ni(Ⅱ) were prepared and characterized by analytical, spectroscopic (IR, UV-Vis, Mass) techniques, electrical conductivity, magnetic and thermal measurements. The crystal and molecular structure of [Cu(HL)2Cl2] was determined by a single-crystal X-ray diffraction study. The molecular structure of the title compound has an inversion center on the Cu atom.展开更多
An efficient and simple procedure for the synthesis of novel isatin derivatives is described. Michael addition of aniline Schiff bases of isatin or p-toluidine Schiff bases of isatin to fumaric esters affords the Mich...An efficient and simple procedure for the synthesis of novel isatin derivatives is described. Michael addition of aniline Schiff bases of isatin or p-toluidine Schiff bases of isatin to fumaric esters affords the Michael adduct com- pounds in good to high yields in the presence of K2CO3 and tetrabutylammonium bromide (TBAB) under sol- vent-free conditions. Repeating of this reaction about spiro[l,3-dioxolane-2,3'-indol]-2'(l'H)-one, as a Michael do- nor, in the presence of 1,4-diazabicyclo[2.2.2]octane (DABCO) gives Michael adducts in remarkable yields under the same conditions.展开更多
Based on the existing reports on the bioactive isatin derivatives, a number of Schiff bases were synthesized by reacting 5-substituted isatins with bioactive amines/hydrazides and their structures were confirmed using...Based on the existing reports on the bioactive isatin derivatives, a number of Schiff bases were synthesized by reacting 5-substituted isatins with bioactive amines/hydrazides and their structures were confirmed using spectroscopic methods such as NMR, IR and mass spectrometry. Furthermore, Nbenzylation of isatin followed by the Schiff base formation furnished a new series of compounds(11a-13c) which allowed the analysis of the effect of isatin N-substitution on the bioactivity of the resulting compounds. The antibacterial activity of the synthesized derivatives was evaluated using a microtiter plate method on a series of gram positive and gram negative bacterial strains. Compounds 2d, 3b, 5c and 6a were among the most potent derivatives against Pseudomonas aeruginosa(MIC = 6.25 μg/m L).Analysis of the structure-activity relationship showed that the incorporation of(thio)urea-based Schiff bases lead to more potent derivatives with a broader spectrum of antibacterial activity. In addition,highly lipophilic compounds such as 11a-12c did not show any measurable antibacterial activity, which implies that an optimal lipophilicity might be an important requirement for the antibacterial activity of the studied isatins. Finally, the finding that hydantoin derivatives of N-benzylisatins(13a-13c) still exhibit some antibacterial activity prompted us to consider exploring the bioactivity of more diverse derivatives of isatin-aminohydantoin Schiff bases(compounds 1a-1d) in our future studies.展开更多
A series of 5-substitued-3-(5-(4-(furan-2-yl)-6-methyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-1,3,4-thiadiazol-2- ylimino)indolin-2-one derivatives were synthesized,characterized and were screened for an...A series of 5-substitued-3-(5-(4-(furan-2-yl)-6-methyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-1,3,4-thiadiazol-2- ylimino)indolin-2-one derivatives were synthesized,characterized and were screened for anti-bacterial,anti-fungal and antitubercular activity.展开更多
A new fluorescent probe for the detection of Hg2+ was designed and synthesized via attaching N-methylisatin to rhodamine B hydrazide through an imine linkage. In an ethanol-Tris buffer medium, the addition of Hg2+ c...A new fluorescent probe for the detection of Hg2+ was designed and synthesized via attaching N-methylisatin to rhodamine B hydrazide through an imine linkage. In an ethanol-Tris buffer medium, the addition of Hg2+ caused a strong orange fluorescence and a visual color change from colorless to pink. Other coexisting metal ions did not interfere with the detection of Hg2+. The research on the detection of Hg2+ in natural water suggested the possibility of practical applications in environment monitoring. Based on ESI-MS analysis, the Hg2+-sensing mechanism was proposed.展开更多
基金a grant from Shandong Provincial Education Department, No. J08LH54
文摘The present study observed the action of 1H-indole-2, 3-dione (isatin) on Bax protein expression in the substantia nigra of a Parkinson's disease animal model. Parkinson's disease-like behaviors were induced in C57BL/6J mice treated with 1-methyl-4-phenyl-1,2, 3, 6-tetrahydropyridine (MPTP) Bax protein expression was significantly reduced in isatin (100, 200 mg/kg)-pretreated mice. Results demonstrate that isatin plays a neuroprotective role in mice treated with MPTP by down-regulating Bax protein expression.
基金Supported by the National Key Project of Major Infectious Disease of China(No.2008ZX10003-006)the National S&T Major Special Project on Major New Drug Innovation, China(No.2009ZX09301-003)
文摘A series of novel moxifloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity, compared to the parent moxifloxacin, was designed, synthesized and characterized by 1H NMR, MS and HRMS. These derivatives were initially evaluated for their in vitro antimycobacterial activity against M. smegmatis CMCC 93202. Compounds 3a―3f, 5a, 5f and 5j were chosen for the further evaluation of their in vitro activity against Mycobacterium tuberculosis(MTB) H37Rv ATCC 27294 and MDR-MTB 09710. All the target com pounds[minimum inhibitory concentration(MIC): 0.39―〉16 μg/mL] were far more active than rifampin(MIC: 2.0―〉256 μg/mL), but less active than moxifloxacin(MIC: 0.1―1.0 μg/mL) against the three tested strains. The most active compounds 3a and 3c were found to be 2―64 fold more potent than isoniazid and rifampin against M. smegmatis CMCC 93202, 2 fold more potent than rifampin against MTB H37Rv ATCC 27294, and 16―〉64 fold more potent than ethambutol, isoniazid and rifampin against MDR-MTB 09710.
文摘Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecules due to the restricted structural features to serve in the laser desorption/ionization mechanism with a problem of background signals appearing in the low mass region. This paper describes the application of Schiff base derivatives of acylhydrazide and isatin as alternate UV-LDI matrices for the analysis of peptides with significantly low background signals. Thirty one compounds have been successfully employed as matrices for the analysis of low molecular weight (LMW) peptides (α-Cyano-4-hydroxycinnamic acid (HCCA), a preferred choice for peptide analysis.
文摘A new approach to synthesis of 6,7-dimethoxyisatin is reported. 2-nitro-3, 4- dimethoxy mandelonitrile in glacial acetic acid was treated with the solution of stannous chloride in hydrochloric acid to give 6, 7-dimethoxyisatin in a high yield.
基金supported by the China-Australia linkage grant form National Natural Science Foundation (NSFC#20911120022)National 973 program (2010CB126103)
文摘The title compounds(Z)-3-(2-(3-chloropyridin-2-yl)hydrazono)indolin-2-one(A) and 7-bromo-(Z)-3-((4-pyridinyl)carboxlichydrazono)-2-indolinone(B) have been synthesized and structurally determined by elemental analysis and single-crystal X-ray diffraction studies.Compound A(C13H8ClN4O) belongs to the orthorhombic crystal system,space group Pca21 with a = 20.799(4),b = 4.9312(10),c = 11.764(2),V = 1206.6(4)3,Mr = 271.68,Dc = 1.496 g/cm3,μ = 0.313 mm-1,F(000) = 556,Z = 4,the final R = 0.0346 and wR = 0.0831 for 2683 observed reflections with I 2σ(I).Compound B(C14H9BrN4O2) belongs to the triclinic crystal system,space group P1 with a = 6.6834(13),b = 7.0727(14),c = 14.285(3),α = 95.56(3),β = 99.00(3),γ = 102.95(3)°,V = 643.8(2)3,Mr = 345.16,Dc = 1.780 g/cm3,μ = 3.203 mm-1,F(000) = 344,Z = 2,the final R = 0.0487 and wR = 0.1167 for 2334 observed reflections with I 2σ(I).The preliminary herbicidal bioassay reveals that compounds A and B have some inhibition both in vivo and in vitro against AHAS.
基金Supported by the China-Australia Linkage Grant form of National Natural Science Foundation,China(No.20911120022)the National Key Technology Research and Development Program of China(No.2011BAE06B05-3)
文摘Two novel compounds 1-(4-fluorobenzyl)-4-chloro-(Z)-3-benzoylhydrazono-2-indolinone(1) and 1-(4-methoxybenzyl)-(Z)-3-benzoylhydrazono-2-indolinone(2) were synthesized and their crystal structures were determined by single-crystal X-ray diffraction.Compound 1(C22H15ClFN3O2) crystallized in the triclinic system,space group P1·with a=0.94198(19) nm,b=1.4339(3) nm,c=1.5018(3) nm,α=101.58(3)°,β=102.96(3)°,γ=102.73°,V=1.8602(6) nm3,Mr=407.82,Dc=1.456 g/cm3,μ=0.240 mm-1,F(000)=840,Z=4,R1=0.0442 and wR2=0.1064.Compound 2(C23H19N3O3) crystallized in the triclinic system,space group P1·with a=1.0022(2) nm,b=1.0192(2) nm,c=1.0461(2) nm,α=99.86(3)°,β=117.30(3)°,γ=94.13(3)°,V=0.9215(3) nm3,Mr=385.41,Dc=1.389 g/cm3,μ=0.094 mm-1,F(000)=404,Z=2,R1=0.0403 and wR2=0.1142.The preliminary herbicidal activities of the two compounds were also evaluated.
文摘New dibutyltin(IV) complexes of Schiff base derived from 5-chloroindoline-2,3-dione, indoline- 2,3-dione with amino acids (tryptophan, alanine and valine) were synthesized and characterized by elemental analysis, IR, electronic spectra, conductance measurements, and biological activity. The analytical data showed that the Schiff base ligand acts as bidentate towards metal ions via the azomethine nitrogen and carboxylate oxygen by a stoichiometric reaction of M:L (1:2) to form metal complexes. NMR (1H, 13C and 119Sn) spectral data of the ligands and metal complex agree with proposed structures. The conductivity values between 14 - 27 ohm-1cm2mol-1 in DMF imply the presence of non-electrolyte species. 3D molecular modeling and analysis of bond lengths and bond angles have also been conducted for a representative compound, [Bu2Sn(L2)2], to substantiate the proposed structures. Antibacterial results indicate that the metal complexes are more active than the free ligands.
文摘The effects of isatin (2,3-dioxo-indole) and isatin analogues (5-methylisatin, 6-hydroxyisatin, 7-ethylisatin, N-acety- lisatin) were tested on prostaglandin E2 (PGE2)-induced fever in mice and rats. Two modes of administration were tested. Isatin or an analogue was injected simultaneously with PGE2 and the development of fever was tested, or the test compound was given 30 min following PGE2 administration and the effects on the already existing fever were measured, in mice and in rats. Isatin in a dose of 3.12 mg/kg ip was found to block the development of PGE2-induced fever in mice, while in a dose of 12.5 mg/kg ip it attenuated the existing fever. In rats isatin in a dose of 12.5 mg/kg ip blocked fever initiation, and at 25.0 mg/kg ip attenuated existing PGE2-induced fever. In mice, 5-methylisatin in a dose of 0.21 mg/kg ip blocked the initiation of fever, and at 6.72 mg/kg ip attenuated the existing fever. In rats in a dose of 3.36 mg/kg ip it blocked the development of fever, and at 13.44 mg/kg ip attenuated existing PGE2-induced fever. In mice 5,6-dimetylisatin in a dose of 0.02 mg/kg ip both blocked fever initiation and attenuated the existing fever in mice, in rats in a dose of 0.42 mg/kg ip it blocked the initiation of fever, and at 0.21 mg/kg ip attenuated the existing PGE2-induced fever. In mice 6-hydroxyisatin in a dose of 5.2 mg/kg blocked the development of fever, and at 10.4 mg/kg attenuated the existing fever. In rats in a dose of 10.40 mg/kg ip it blocked fever development and also attenuated the existing fever. In mice, 7-ethylisatin in a dose of 0.02 mg/kg ip both blocked fever initiation and also attenuated the existing fever. In rats, a dose of 0.11 mg/kg both blocked fever initiation and also attenuated the existing fever. In mice, N-acethylisatin in the dose of 0.005 mg/kg blocked fever initiation, while at 1.024 mg/kg it attenuated existing fever, in rats, in a dose of 0.096 mg/kg it blocked fever initiation, and at 0.384 mg/kg attenuated the existing fever. The results demonstrate that 7-ethyl- and N-acetylisatin are the most effective of these compounds both in blocking the development of PGE2-induced fever and also in attenuating existing the PGE 2-induced fever.
文摘Schiff base ligand (HL) derived from 4-hexylaniline with isatin (1H-indole-2,3-dione) and its complexes with Cu(Ⅱ), Ni(Ⅱ) were prepared and characterized by analytical, spectroscopic (IR, UV-Vis, Mass) techniques, electrical conductivity, magnetic and thermal measurements. The crystal and molecular structure of [Cu(HL)2Cl2] was determined by a single-crystal X-ray diffraction study. The molecular structure of the title compound has an inversion center on the Cu atom.
文摘An efficient and simple procedure for the synthesis of novel isatin derivatives is described. Michael addition of aniline Schiff bases of isatin or p-toluidine Schiff bases of isatin to fumaric esters affords the Michael adduct com- pounds in good to high yields in the presence of K2CO3 and tetrabutylammonium bromide (TBAB) under sol- vent-free conditions. Repeating of this reaction about spiro[l,3-dioxolane-2,3'-indol]-2'(l'H)-one, as a Michael do- nor, in the presence of 1,4-diazabicyclo[2.2.2]octane (DABCO) gives Michael adducts in remarkable yields under the same conditions.
文摘Based on the existing reports on the bioactive isatin derivatives, a number of Schiff bases were synthesized by reacting 5-substituted isatins with bioactive amines/hydrazides and their structures were confirmed using spectroscopic methods such as NMR, IR and mass spectrometry. Furthermore, Nbenzylation of isatin followed by the Schiff base formation furnished a new series of compounds(11a-13c) which allowed the analysis of the effect of isatin N-substitution on the bioactivity of the resulting compounds. The antibacterial activity of the synthesized derivatives was evaluated using a microtiter plate method on a series of gram positive and gram negative bacterial strains. Compounds 2d, 3b, 5c and 6a were among the most potent derivatives against Pseudomonas aeruginosa(MIC = 6.25 μg/m L).Analysis of the structure-activity relationship showed that the incorporation of(thio)urea-based Schiff bases lead to more potent derivatives with a broader spectrum of antibacterial activity. In addition,highly lipophilic compounds such as 11a-12c did not show any measurable antibacterial activity, which implies that an optimal lipophilicity might be an important requirement for the antibacterial activity of the studied isatins. Finally, the finding that hydantoin derivatives of N-benzylisatins(13a-13c) still exhibit some antibacterial activity prompted us to consider exploring the bioactivity of more diverse derivatives of isatin-aminohydantoin Schiff bases(compounds 1a-1d) in our future studies.
文摘A series of 5-substitued-3-(5-(4-(furan-2-yl)-6-methyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-1,3,4-thiadiazol-2- ylimino)indolin-2-one derivatives were synthesized,characterized and were screened for anti-bacterial,anti-fungal and antitubercular activity.
基金Supported by the National Natural Science Foundation of China(No.21162010).
文摘A new fluorescent probe for the detection of Hg2+ was designed and synthesized via attaching N-methylisatin to rhodamine B hydrazide through an imine linkage. In an ethanol-Tris buffer medium, the addition of Hg2+ caused a strong orange fluorescence and a visual color change from colorless to pink. Other coexisting metal ions did not interfere with the detection of Hg2+. The research on the detection of Hg2+ in natural water suggested the possibility of practical applications in environment monitoring. Based on ESI-MS analysis, the Hg2+-sensing mechanism was proposed.