Synthesis, Characterization And Biological Screening Of Metal Complexes With Some Heterocyclic Ligands (original) (raw)
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Applied Organometallic …, 2009
, copper(II), nickel(II) and zinc(II)] have been synthesized and characterized. The nature of bonding and structure of all the synthesized compounds have been proposed from magnetic susceptibility and conductivity measurements, IR, 1 H and 13 C NMR, electron spectra, mass spectrometry and CHN analysis data. The structure of ligand, 4-{[(E)-(5-chloro-2-hydroxyphenyl) methylidene] amino}-N-(4,6-dimethyl pyrimidin-2-yl) benzene sulfonamide has also been determined by X-ray diffraction method. An octahedral geometry has been suggested for all the complexes. The ligands and metal complexes have been screened for their in vitro antibacterial, antifungal and cytotoxic activity. The results of these studies revealed that all compounds showed moderate to significant antibacterial activity against one or more bacterial strains and good antifungal activity against various fungal strains.
Metal Complexes of Heterocyclic Sulphonamide: Synthesis, Characterization and Biological Activity
The metal complex of heterocyclic sulphonamide with aminopyridine is a substantial class of pharmaceutical drugs used to treat infection, diabetes, anti-inflammatory issues and neurological disorders in the field of medicinal chemistry. The research reports the synthesis, characterization and biological activity of metal complexes of heterocyclic sulphonamide of aminopyridine. Sulphonamide of heterocyclic pyridine was synthesized by reacting 2-aminopyridine and tosyl chloride in an aqueous alkaline solution at ambient temperature. The iron (II) and copper (II) complexes of the ligand were also synthesized and recrystallized with suitable solvents, and the purity levels were ascertained with melting point and thin layer chromatographic pattern. Structural elucidation of the compounds was done via Nuclear Magnetic Resonance (NMR), Ultraviolet-Visible Spectroscopy (UV-VIS) Infrared (IR), Electrospray Ionization Mass Spectrometry (ESI-MS) Micro elemental analysis. Some absorption bands in the IR spectrum of heterocyclic sulphonamide derivatives were found to shift either to higher or lower wavenumbers in the complexes, indicating the involvement of azomethine nitrogen in coordination with the metal ion. The synthesized ligand and its metal complexes were screened for antimicrobial activity against Gram (-) Escherichia coli, Gram (-) Salmonella typhi, Gram (+) Staphylococcus aureus, Aspergillus flavus, Aspergillus niger and Saccharomyces cerevisiae. The ligand did not show activity against the selected bacterial and fungal strains whereas; some of the coordinated ligands gave a substantial improvement on their bactericidal and fungicidal activity. The complex of copper (II) was not bioactive to all the bacteria strains but sensitive to all the fungi strains. The complex of iron (II) was susceptible to the bacteria and fungi strains, except Aspergillus flavus that was inactive. When compared to Ciprofloxacin and Ketoconazole, with a broad-spectrum antibiotic, the standard antimicrobial agents were better in sensitivity than the synthesized compound.
Synthesis of Sulfonamides, Metal Complexes and the Study of In vitro Bio-
A modified method for the synthesis of a series of substituted benzenesulfonamides from benzenesulfonylchlo- ride and substituted amines (1:1) in aqueous media have been adopted at controlled pH (8-10). Transition metal com- plexes of synthesized ligands were also prepared by refluxing ligands and metal salts (2:1) for one hour. The synthesized compounds have been characterized by spectroscopic techniques (FTIR, 1 HNMR and mass spectrometry). Synthesized compounds were analyzed for their activity toward acetyl cholinesterase (AChE) inhibition, butyrylcholinesterase (BChE) inhibition, lipoxygenase (LOX) inhibition, antioxidant (DPPH) and antiurease. As regards biological activities of ligands, only N-(2-nitrophenyl) benzenesulfonamide (3) showed appreciated value of IC 50 = 77.13± 00 mole against LOX while all metal complexes showed low activities. Cu complex (C-4) showed moderate activity against LOX while all the other metal complexes had no activity against any enzyme at all. Similarly Zn complexes (Z-2 to Z-6) showed little activity against AChE but the ligands showed no significant activity against any other. Metal complexes showed high capacity toward antiurease activity.
Schiff base namely 4-((thiophene-2-yl) methyleneamino) phenyl sulfonamide (L) and its Co (II), Ni (II), Cu (II) and Zn (II) complexes were synthesized and characterized by UV-Vis, IR, 1H-NMR, MS-EI, elemental analysis and TGA. Molar conductance and Magnetic susceptibility of the complexes were also analyzed. Elemental analyses confirmed a 2:1 molar ratio of ligand to metal ion of the complexes. IR spectra revealed that L is coordinated to the metal ions through azomethine-N and Thiophene-S. On the basis of experimental data octahedral geometry was proposed for all complexes. Thermal studies together with IR showed the presence of lattice and coordinated water molecules in all complexes. The in vitro antimicrobial activities of the compounds were tested against S.aureus, K.pneumoniae , C. albicans and C.krusei by the agar well diffusion assay. The result indicated that the ligand become antimicrobially active on chelation with metal ions. It was found that Cu(II) complex showed the highest antibacterial activity among all complexes.
2012
sulfonamide (sulfadiazine) with some N-alkyl-N-phenyl dithiocarbamate have been synthesized and characterized by elemental analysis, conductivity measurements, UV-Vis and FTIR spectroscopy. The complexes are formulated as four coordinate MN2S2 species in which the metal ions are coordinated to one molecule of sulfadiazine through the pyrimidinyl and sulfulnamido nitrogen atoms and one molecule of dithiocarbamate through two sulfur atoms with both molecules acting as bidentate chelating ligands. The in vitro antibacterial activities of the complexes and sulfadiazine were evaluated against eight bacteria strains using the agar well diffusion method. The metal complexes showed varied antibacterial properties and their minimum inhibitory concentration (MIC) and maximum bactericidal concentration (MBC) were determined.
World Scientific News, 2020
A novel series of Sulfonamide embedded heterocyclic derivatives were synthesized and well characterized by using 1 H NMR, 13 C NMR and IR spectroscopic techniques. All the new synthesized compounds were evaluated to their anti-bacterial, anti-fungal and anti-malarial activities. Noticeably, compound 5b was the most potent compound in vitro anti-microbial (S. aureus) with a MTCC value of 96 microgram/ml and compounds 5g and 5j showed most potent activity in vitro anti-fungal (C. albicans) with a MTCC value of 277microgram/ml. Similarly, compound 5e showed high potent activity of antimalarial (P. falciparum) with mean IC50 value as compared to other synthesized derivatives.
a Biologically Active Sulfonamide Moiety
2014
Abstract: This study aimed for the synthesis of new heterocyclic compounds incorporating sulfamoyl moiety suitable for use as antimicrobial agents via a versatile, readily accessible N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide (3). The 2-pyridone derivatives were obtained via reaction of cyanoacetamide with acetylacetone or arylidenes malononitrile. Cycloaddition reaction of cyanoacetamide with salicyaldehyde furnished chromene derivatives. Diazotization of 3 with the desired diazonium chloride gave the hydrazone derivatives 13a–e. Also, the reactivity of the hydrazone towards hydrazine hydrate to give Pyrazole derivatives was studied. In addition, treatment of 3 with elemental sulfur and phenyl isothiocyanate or malononitrile furnished thiazole and thiophene derivatives respectively. Reaction of 3 with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt 17 which reacted in situ with 3-(2-bromoacetyl)-2H-chromen-2-one and methyl iodide afforded the thiazole and kete...
RSC Adv., 2015
The present study reports the synthesis of Zn(II) complexes of tosyl sulfonamide derivatives obtained by the reaction of tosyl chloride with L-amino acids. The ligands and their complexes were characterized by IR, 1 H and 13 C-NMR, GC-MS, elemental analysis and X-ray crystallography in the case of NA3. All compounds were screened for their carbonic anhydrase inhibitory activities. Results demonstrated that complexes are stronger inhibitors of carbonic anhydrase compared to their parent ligands, which warrants further development of organometallics as active carbonic anhydrase inhibitors. Cytotoxicity assays on lung carcinoma (H-157) and kidney fibroblast (BHK-21) cancer cells demonstrated that compounds were potent anticancer agents. Additionally, the complexes were screened against promastigote forms of Leishmania major and found to be significant antileishmanial agents. Molecular docking studies were performed against bCA II enzymes to rationalize the inhibitory properties of these compounds. The identified inhibitors showed promise for the design of interesting pharmacological agents.
The present study reports the synthesis of Zn(II) complexes of tosyl sulfonamide derivatives obtained by the reaction of tosyl chloride with L-amino acids. The ligands and their complexes were characterized by IR, 1 H and 13 C-NMR, GC-MS, elemental analysis and X-ray crystallography in the case of NA3. All compounds were screened for their carbonic anhydrase inhibitory activities. Results demonstrated that complexes are stronger inhibitors of carbonic anhydrase compared to their parent ligands, which warrants further development of organometallics as active carbonic anhydrase inhibitors. Cytotoxicity assays on lung carcinoma (H-157) and kidney fibroblast (BHK-21) cancer cells demonstrated that compounds were potent anticancer agents. Additionally, the complexes were screened against promastigote forms of Leishmania major and found to be significant antileishmanial agents. Molecular docking studies were performed against bCA II enzymes to rationalize the inhibitory properties of these compounds. The identified inhibitors showed promise for the design of interesting pharmacological agents.