SYNTHESIS, CHARACTERIZATION, DNA CLEAVAGE AND ANTIMICROBIAL ACTIVITIES OF SCHIFF BASE LIGAND DERIVED FROM 5-CHLORO-3-PHENYL-1H-INDOLE-2-CARBOXYHYDRAZIDE AND O-VANILLIN AND ITS METAL (II) COMPLEXES

Objective: The main objective of the present work was to synthesize a new Schiff base ligand 5-chloro-N'-(2-hydroxy-3-methoxybenzylidene)-3-phenyl-1H-indole-2-carbohydrazide and its Cu (II), Co (II), Ni (II) and Zn (II) complexes and study their biological activity.Methods: The compounds are characterized by elemental analysis and various physicochemical techniques like IR, 1H NMR, ESI-mass, UV-Visible, TGA analyzes and molar conductance data. All the compounds were screened for their antibacterial and antifungal activity by MIC method. Further, antioxidant activity was performed by using 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and DNA cleavage activity by Agarose Gel Electrophoresis (AGE) method.Results: Spectral investigations suggested octahedral coordination geometrical arrangement for all the metal (II) complexes, having 1:2 stoichiometric ratio of the type [M(L)2]. The antimicrobial activity results revealed that the metal complexes were found to be more active than the free ligand. Furthermore, the DNA cleavage activity of the compounds on plasmid DNA pBR322 molecule showed moderate activity.Conclusion: The newly synthesized ligand acts as ONO donor tridentate chelate and coordinated through an oxygen atom of carbonyl function, azomethine nitrogen and phenolic oxygen atom to the Cu, Co, Ni and Zn metal ions and form octahedral geometrical arrangement. All the complexes are found to be non-electrolytic in nature. Further, all the newly prepared compounds showed moderate biological activity.Keywords: Indole, o-Vanillin, Transition metal complexes, Powder XRD, ESR, DNA cleavage Antimicrobial, AntioxidantÂ

Synthesis, Characterization, Antimicrobial, DNA Cleavage, and In Vitro

A novel Schiff base ligand N-(4-phenylthiazol-2yl)-2-((2-thiaxo-1,2-dihydroquinolin-3-yl)methylene)hydrazinecarboxamide (L) obtained by the condensation of N-(4-phenylthiazol-2-yl)hydrazinecarboxamide with 2-thioxo-1,2-dihydroquinoline-3-carbaldehyde and its newly synthesized Cu(II), Co(II), Ni(II), and Zn(II) complexes have been characterized by elemental analysis and various spectral studies like FT-IR, 1H NMR, ESI mass, UV-Visible, ESR, TGA/DTA, and powder X-ray diffraction studies. The Schiff base ligand (L) behaves as tridentate ONS donor and forms the complexes of type [ML(Cl)2] with square pyramidal geometry. The Schiff base ligand (L) and its metal complexes have been screened in vitro for their antibacterial and antifungal activities by minimum inhibitory concentration (MIC) method. The DNA cleavage activity of ligand and its metal complexes were studied using plasmid DNA pBR322 as a target molecule by gel electrophoresis method. The brine shrimp bioassay was also carried out to study the in vitro cytotoxicity properties for the ligand and its metal complexes against Artemia salina. The results showed that the biological activities of the ligand were found to be increased on complexation

Synthesis and pharmacological activity of 2H-3-(various substituted indol-2'-carboxamidyl)-3,4-dihydro-1,3-benzoxazines and 2H-3-(2',5'-disubstituted indol-3'-yl)methyl-1,3-benzoxazoles

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Razvoj i validacija spektrofotometrijskih metoda za određivanje ceftazidima u farmaceutskim doziranim pripravcima

Two spectrophotometric methods for the determination of ceftazidime (CFZM) in either pure form or in its pharmaceutical formulations are described. The first method is based on the reaction of 3-methylbenzothiazolin-2-one hydrazone (MBTH) with ceftazidime in the presence of ferric chloride in acidic medium. The resulting blue complex absorbs at λmax 628 nm. The second method describes the reaction between the diazotized drug and N-(1-naphthyl)ethylenediamine dihydrochloride (NEDA) to yield a purple colored product with λmax at 567 nm. The reaction conditions were optimized to obtain maximum color intensity. The absorbance was found to increase linearly with increasing the concentration of CFZM; the systems obeyed the Beer’s law in the range 210 and 1050 µg mL1 for MBTH and NEDA methods, respectively. LOD, LOQ and correlation coefficient values were 0.15, 0.79 and 0.50, 2.61. No interference was observed from common excipients present in pharmaceutical formulations. The proposed methods are simple, sensitive, accurate and suitable for quality control applications.Razvijene su dvije spektrofotometrijske metode za određivanje ceftazidima (CFZM), čistog ili u farmaceutskim pripravcima. Prva metoda se temelji na reakciji 3-metilbenzotiazolin-2-on hidrazona (MBTH) sa ceftazidimom u prisutnosti željezovog(III) klorida u kiselom mediju. Nastaje plavi kompleks s maksimumom apsorpcije pri λmax 628 nm. Druga metoda se temelji na reakciji između diazotiranog lijeka i N-(1-naftil)etilendiamin dihidroklorida (NEDA), pri čemu nastaje ljubičasti produkt s λmax pri 567 nm. Reakcijski uvjeti su optimirani da se dobije maksimalni intenzitet boje. Apsorbancija raste linearno s porašću koncentracije CFZM; sustavi slijede Beerov zakon u koncentracijskom području 210 za MBTH metodu i 1050 µg mL1 za NEDA metodu. LOD i LOQ te vrijednosti korelacijskog koeficijenta su 0,15, 0,79 i 0,50, 2,61. Uobičajene pomoćne tvari ne smetaju određivanju ceftazidima. Predložene metode su jednostavne, osjetljive, točne i pogodne za primjenu u kontroli kvalitete

Synthesis, spectral characterization and biological activity studies of transition metal complexes of Schiff base ligand containing indole moiety

<div><p>A new series of transition metal complexes of Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II), with a tridentate (oxygen nitrogen nitrogen) ligand 3,5-dimethyl-<i>N</i>^′-[(1<i>E</i>)-1^′-pyridin-2^′-ylethylidene]-1<i>H</i>-indole-2-carbohydrazide (<b>L</b>) have been synthesized and characterized on the basis of analytical, magnetic susceptibility, infra red, nuclear magnetic resonance, fast atom bombardment-mass, electron paramagnetic resonance spectral studies, X-ray powder diffraction and UV-visible spectral data. Based on analytical and molar conductance data, the complexes may be formulated as [M(L)₂]·(H₂O)_<i>n</i>, where M˭ Co, Cu and Ni and [M(L)Cl₂].(H₂O)_<i>n</i>, where M=Zn, Cd and Hg. The spectral studies revealed that, an octahedral geometry for Co(II), Ni(II) and Cu(II) complexes, whereas square pyramidal geometry for Zn(II), Cd(II) and Hg(II) complexes. The ligand and its Co(II) complex have been characterized by X-ray powder diffraction studies. The ligand and its complexes were tested for their antibacterial activity against <i>Escherichia coli</i> & <i>Staphyloccocus aureus</i> and antifungal activity against <i>Aspergillus niger</i> & <i>Candida albicans</i>.</p></div