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Standard Drug (standard + drug)
Selected AbstractsEffect of aqueous extract of Tragia involucrata Linn. on acute and subacute inflammationPHYTOTHERAPY RESEARCH, Issue 4 2006Ramar Perumal Samy Abstract Antiinflammatory activity of aqueous extract of Tragia involucrata was tested on carrageenan-induced hind paw oedema and cotton pellet granuloma models in albino rats. In the subacute model, cotton pellet granuloma was produced by implantation of 10 mg sterile cotton in the axilla under ether anaesthesia. The animals were administered an aqueous extract at various concentrations of 50, 100, 200, 300 and 400 mg/kg. Phenyl butazone (80 mg/kg) was used as a standard drug. The paw diameter was measured at different time intervals and the dry granuloma weight was taken after the treatment. The aqueous leaf extract (400 mg/kg) showed the maximum inhibition (84.23%) of oedema at the end of 3 h following carrageenin-induced rat paw oedema. In subacute inflammation, the extract showed 76.25% reduction in granuloma weight. The results prove that the aqueous leaf extract showed highest antiinflammatory activity in acute and subacute inflammation and also support the usage of traditional claims. Copyright © 2006 John Wiley & Sons, Ltd. [source] In-vitro antimicrobial, thermal and spectral studies of mixed ligand Cu(II) heterochelates of clioquinol and coumarin derivativesAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 4 2010G. J. Kharadi Abstract The mixed-ligand heterochelates of Cu(II) with 5-chloro-7-iodo-8-hydroxyquinoline (clioquinol) and various uninegative bidentate ligands were prepared. The structure of mixed-ligand heterochelates was investigated using spectral, physicochemical, elemental analysis and thermal studies. The FAB-mass spectrum of [Cu(A2)(CQ)(H2O)2].2H2O has been carried out. Magnetic moment and reflectance spectral studies reveal that an octahedral geometry has been assigned to all the prepared heterochelates. The kinetic parameters such as order of reaction (n), the energy of activation (Ea), the pre-exponential factor (A), the activation entropy (,S#), the activation enthalpy (,H#) and the free energy of activation (,G#) have been reported. The ligands, metal salts, heterochelates, control and standard drug were tested for their in-vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Serratia marcescens and Bacillus substilis. The metal complexes exhibit good activity against bacterial strains compared with parental compounds, and moderate compared with the standard drug (clioquinol). Copyright © 2010 John Wiley & Sons, Ltd. [source] Palladium(II) and platinum(II) complexes of (1R,2R)-(,)-1,2-diaminocyclohexane (DACH) with various carboxylato ligands and their cytotoxicity evaluationAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 5 2009Talal A.K. Al-Allaf Abstract Several palladium(II) and platinum(II) complexes analogous to oxaliplatin, bearing the enantiomerically pure (1R,2R)-(,)-1,2-diaminocyclohexane (DACH) ligand, of the general formula {MX2[(1R,2R)-DACH]}, where M = Pd or Pt, X (COO)2, CH2(COO)2, , , {1,1,-C5H8(CH2COO)2}, [1,1,-C6H10(CH2COO)2], [1,1,-(COO)2ferrocene], , , , MeCOO and Me3CCOO, were synthesized. All the complexes prepared were characterized physicochemically and spectroscopically. Some selected complexes were screened in vitro against several tumor cell lines and the results were compared with reference standard drug, oxaliplatin. Copyright © 2009 John Wiley & Sons, Ltd. [source] Synthesis and Anti-Inflammatory Activity of Novel (4-Hydroxyphenyl)(2,4-dimethoxyphenyl) Methanone DerivativesARCHIV DER PHARMAZIE, Issue 8 2009Kambappa Vinaya Abstract In the scope of the research program aiming to perform the synthesis and pharmacological evaluation of novel possible anti-inflammatory compounds, in this manuscript, we report the synthesis of novel carboxamide 9a - d and thioamide 10a - d derivatives from the benzophenone and piperidine nucleus. Variation in the functional group at the N -terminal of piperidine led to two sets of compounds, bearing the carboxamide and thioamide, respectively. The characterization of this new class of compounds was performed with 1H-NMR, LC-MS, IR, and elemental analysis. The newly synthesized compounds were screened for their anti-inflammatory activity by carrageenan-induced foot pad oedema assay and were compared with a standard drug. All the compounds exhibited anti-inflammatory activity at the dose of 30 mg/kg p.o. with varying degree from 52 to 67% inhibition of oedema. The compounds 9d and 10d with dichloro and fluoro substitution showed more potent activity at 30 mg/kg p.o. than the standard drug. [source] Synthesis and Biological Evaluation of Novel 4-Substituted 1-{[4-(10,15,20-Triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazides as New Class of Potential Antiprotozoal AgentsCHEMISTRY & BIODIVERSITY, Issue 5 2008Abdul Abstract A novel series of 4-substituted 1-{[4-(10,15,20-triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazide, 4a,4n, was synthesized in 9,21% yield by the condensation of 4-(10,15,20-triphenylporphyrin-5-yl)benzaldehyde (3) with various substituted thiosemicarbazides in presence of catalytic amount of AcOH. These compounds were assayed for in vitro antiamoebic activity, and the results showed that out of 14 compounds 9 were found with IC50 values lower than metronidazole corresponding to 1.05- to 4.7-fold increase in activity. MTT Assay showed that all the compounds are nontoxic to human kidney epithelial cell line. 4-(m -Toluidinyl)-1-{[4-(10,15,20-triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazide (4h) showed the highest antiamoebic activity with least cytotoxicity. Some of the compounds were screened for their antimalarial activities and ability to inhibit , -haematin formation, but none of them showed an activity better than chloroquine and quinine. Only one compound out of six showed an activity comparable to standard drug. [source] Synthesis, spectroscopy, thermal and biological aspect of novel six-coordinated dimeric iron(III) mixed-ligand complexesAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 8 2008M. N. Patel Abstract The mixed-ligand complexes of iron(III) with 1-cyclopropyl-6-fluoro-4-oxo-7-piperazin-1-yl-1,4-dihydroquinoline-3-carboxylic acid and various neutral bidentate Schiff base ligands were prepared. The structure of mixed-ligand complexes was investigated using spectral, physicochemical and elemental analyses. Biocidal activity was determined using agar plate technique against Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Salmonella typhi, Escherichia coli and Serratia marcescens. The result showed a significant increase in a biocidal activity compared with parent ligands, metal salts and standard drugs (ofloxacin, levofloxacin). DNA binding and cleavage studies were carried out using absorption titration and gel electrophoresis techniques, respectively. The binding constant of Fe(III) complexes was obtained in the range 2.5,4.0 × 104M,1. The DNA binding and cleavage efficacy were raised in mixed-ligand complexes as compared with parental ligands and metal salts. Copyright © 2008 John Wiley & Sons, Ltd. [source] Synthesis and Evaluation of Novel Indolylthiadiazinoazetidinones and Indolylthiadiazinothiazolidinones as Antimicrobial AgentsARCHIV DER PHARMAZIE, Issue 2 2010Vikas Kumar Abstract Some new 5-methoxy/ethoxy-2,3-[2,-(3,,-chloro-2,,-oxo-4,,-substituted-aryl-1,,-azetidinyl)-1,,3,,4,-thiadiazino]indoles 13,20 and 5-methoxy/ethoxy-2,3-[2,-(2,,-substituted-aryl-4,,-oxo-1,,,3,,-thiazolidin-3,,-yl)-1,,3,,4,-thiadiazino]indoles 21,28 have been synthesized from 5-methoxy/ethoxy-2,3-[2,-(substituted-benzylidinylimino)-1,,3,,4,-thiadiazino]indoles 5,12. These newly synthesized compounds were characterized by elemental and spectral analysis. Further, compounds 5,28 of the present series have been screened for their antibacterial and antifungal activities. Both minimal inhibitory concentration (MIC) and inhibition zones were determined in order to monitor the efficacy of the synthesized compounds. Compounds 14 and 16 were found to be the most potent members of the present series, they showed maximal antibacterial and antifungal properties much better than the standard drugs. [source] | ||||||||||