Two novel copper complexes (<strong>1,2</strong>) with N,O-donor ligands were synthesized by reaction of copper(II) malonates with 3,3’-bis(pyrazolyl)pentane and 4,4’-trimethylenedipyridine in methanol a...Two novel copper complexes (<strong>1,2</strong>) with N,O-donor ligands were synthesized by reaction of copper(II) malonates with 3,3’-bis(pyrazolyl)pentane and 4,4’-trimethylenedipyridine in methanol at moderate temperature. These compounds were characterized by elemental analysis, UV-VIS, IR spectroscopies and powder X-ray diffraction analyses. Compound (<strong>1</strong>) melts at higher temperature (202°C) than compound (<strong>2</strong>) (100<span style="white-space:normal;">°</span>C). The IR spectra showed typical vibrations related to C=N and C=C, characteristic of pyrazolyl and pyridine ligands.展开更多
The title complex[Zn_2L(C_5H_7N_2)_2(C_5H_7N_2·HClO_4)_2](L=1,2-di(3', 5'-dimethylpyrazolyl) formylhydrazine and C_5H_7N_2= 3 , 5 dimethylpyrazole anion) has been synthesized by template reaction, in whic...The title complex[Zn_2L(C_5H_7N_2)_2(C_5H_7N_2·HClO_4)_2](L=1,2-di(3', 5'-dimethylpyrazolyl) formylhydrazine and C_5H_7N_2= 3 , 5 dimethylpyrazole anion) has been synthesized by template reaction, in which carbonhydrazine, 2, 4-pentanedione and zinc perchlorate hexahydrate were used as the original materials. The crystals of complex with formula C_(32)H_(46)N_(14)O_(10)Cl_2Zn_2 (Mr=988.46) are triclinic,space group P1,a= 8.275 (2),b=11.523 (3),c= 12.872(5), a=69. 90(3),β= 69.79 (2), γ=83. 52 (2)°,V=1081.6(6),Z=1,Dc=1.524g/cm￣3,μ=13.265cm￣(-1),F (000)=510. The final refinement is converged with R= 0.057. The results indicate that in one complex molecule there are three kinds of pyrazole rings all directly coordinated to the central Zn atom; and each zinc atom possesses a five-coordinated polyhedron.展开更多
p38α mitogen activated protein kinase(MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders.A series of fifteen pyrazolyl urea derivatives(3a-o) were synthesized and evaluated for thei...p38α mitogen activated protein kinase(MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders.A series of fifteen pyrazolyl urea derivatives(3a-o) were synthesized and evaluated for their p38α MAPK inhibition and antioxidant potential.Compounds 3a-e,3g and 3h showed low micromolar range potency(IC_(50) values ranging from 0.037 ±1.56 to 0.069± 0.07μmol/L)compared to the standard inhibitor SB 203580(IC_(50) = 0.043 + 3.62μmol/L) when evaluated for p38αMAPK inhibition by an immunosorbent-based assay.Antioxidant activity was measured by a 2,2'-diphenyl-1-picryl hydrazyl radical(DPPH) free radical scavenging method and one of the compounds,3c,showed better percentage antioxidant activity(75.06%) compared to butylated hydroxy anisole(71.53%)at 1 mmol/L concentration.Compounds 3a-e,3g and 3h showed promising in vivo anti-inflammatory activity(ranging from 62.25%to 80.93%) in comparison to diclofenac sodium(81.62%).The ulcerogenic liability and lipid peroxidation activity of these compounds were observed to be less in comparison to diclofenac sodium.These compounds also potently inhibited the lipopolysaccharide(LPS)-induced TNF-αrelease in mice(ID_(50) of 3a-c = 19.98,11.32 and 9.67 mg/kg,respectively).Among the screened compounds,derivative 3c was found to be the most potent and its binding mode within the p38α MAPK is also reported.展开更多
文摘Two novel copper complexes (<strong>1,2</strong>) with N,O-donor ligands were synthesized by reaction of copper(II) malonates with 3,3’-bis(pyrazolyl)pentane and 4,4’-trimethylenedipyridine in methanol at moderate temperature. These compounds were characterized by elemental analysis, UV-VIS, IR spectroscopies and powder X-ray diffraction analyses. Compound (<strong>1</strong>) melts at higher temperature (202°C) than compound (<strong>2</strong>) (100<span style="white-space:normal;">°</span>C). The IR spectra showed typical vibrations related to C=N and C=C, characteristic of pyrazolyl and pyridine ligands.
文摘The title complex[Zn_2L(C_5H_7N_2)_2(C_5H_7N_2·HClO_4)_2](L=1,2-di(3', 5'-dimethylpyrazolyl) formylhydrazine and C_5H_7N_2= 3 , 5 dimethylpyrazole anion) has been synthesized by template reaction, in which carbonhydrazine, 2, 4-pentanedione and zinc perchlorate hexahydrate were used as the original materials. The crystals of complex with formula C_(32)H_(46)N_(14)O_(10)Cl_2Zn_2 (Mr=988.46) are triclinic,space group P1,a= 8.275 (2),b=11.523 (3),c= 12.872(5), a=69. 90(3),β= 69.79 (2), γ=83. 52 (2)°,V=1081.6(6),Z=1,Dc=1.524g/cm￣3,μ=13.265cm￣(-1),F (000)=510. The final refinement is converged with R= 0.057. The results indicate that in one complex molecule there are three kinds of pyrazole rings all directly coordinated to the central Zn atom; and each zinc atom possesses a five-coordinated polyhedron.
基金Department of Science and Technology,Women Scientists Scheme-A(File No.SR/WOS-A/CS-84/2013),New Delhi,for providing financial assistance
文摘p38α mitogen activated protein kinase(MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders.A series of fifteen pyrazolyl urea derivatives(3a-o) were synthesized and evaluated for their p38α MAPK inhibition and antioxidant potential.Compounds 3a-e,3g and 3h showed low micromolar range potency(IC_(50) values ranging from 0.037 ±1.56 to 0.069± 0.07μmol/L)compared to the standard inhibitor SB 203580(IC_(50) = 0.043 + 3.62μmol/L) when evaluated for p38αMAPK inhibition by an immunosorbent-based assay.Antioxidant activity was measured by a 2,2'-diphenyl-1-picryl hydrazyl radical(DPPH) free radical scavenging method and one of the compounds,3c,showed better percentage antioxidant activity(75.06%) compared to butylated hydroxy anisole(71.53%)at 1 mmol/L concentration.Compounds 3a-e,3g and 3h showed promising in vivo anti-inflammatory activity(ranging from 62.25%to 80.93%) in comparison to diclofenac sodium(81.62%).The ulcerogenic liability and lipid peroxidation activity of these compounds were observed to be less in comparison to diclofenac sodium.These compounds also potently inhibited the lipopolysaccharide(LPS)-induced TNF-αrelease in mice(ID_(50) of 3a-c = 19.98,11.32 and 9.67 mg/kg,respectively).Among the screened compounds,derivative 3c was found to be the most potent and its binding mode within the p38α MAPK is also reported.
