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Pharmacological reports: PR 12/2012; · 2.44 Impact Factor
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ABSTRACT: A new series of hydrazone and bishydrazone derivatives was synthesized starting from adipic dihydrazide, oxalyl dihydrazide,
4-hydroxybenzhydrazide, 2-furancarboxylic acid hydrazide, acetohydrazide, 4-pyridinecarboxylic acid hydrazide, and isatin.
The chemical structures were confirmed by means of 1H-NMR, UV, and IR spectral data and elemental analysis. The synthesized compounds were evaluated in vitro as antimicrobial
agents against representative strains of Gram-positive (clinical strains of Staphylococcus saprophyticus, Bacillus cereus, Enterococcus faesium), Gram-negative bacteria (clinical strains of Klebsiella pneumonia, Escherichia coli, Serratia marcescens, Pseudomonas aeruginosa, Shigella dysenteriae, Salmonella typhi), and antifungal agent against Candida albicans (clinical isolated) by the minimal inhibitory concentration (MIC) method. MIC was defined as the lowest concentration of
compound inhibiting the growth of each strain. All the bacteria and fungi studied were screened against some antibiotics and
their chemical zone diameters compared.
Keywordsisatin-antibacterial activity-hydrazone derivatives-bishydrazone derivatives
Pharmaceutical Chemistry Journal 04/2012; 44(4):219-227. · 0.37 Impact Factor
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ABSTRACT: Isatin-3-isonicotinylhydrazone was synthesized and characterized. The interaction of native calf thymus DNA with isatin-3-isonicotinylhydrazone (IINH) in 10 mM Tris-HCl aqueous solutions at neutral pH 7.4 has been investigated by spectrophotometric, circular dichroism (CD), melting temperature (T ( m )), spectrofluorimetric, and viscometric techniques. It is found that IINH molecules could intercalate between base pairs of DNA as are evidenced by: hypochromism in UV absorption band of IINH, induced CD spectral changes, sharp increase in specific viscosity of DNA, and increase in the fluorescence of methylene blue (MB)-DNA solutions in the presence of increasing amounts of IINH, which indicates that it is able to release the intercalated MB completely. The binding constants of IINH-DNA complex at four different temperatures (277, 288, 298, and 310 K) were calculated to be 4.7 × 10(4), 2.2 × 10(4), 1.75 × 10(4) and 1.1 × 10(4) M(-1), respectively. Furthermore, the enthalpy and entropy of the reaction between IINH and CT-DNA showed that the reaction is enthalpy-favored and entropy- disfavored (∆H = -30.187 kJ mol(-1); ∆S = -20.46 J mol(-1)K(-1)) which are other evidences to indicate the IINH is able to be intercalated in the DNA base pairs.
Molecular Biology Reports 07/2011; 39(4):3853-61. · 2.93 Impact Factor
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ABSTRACT: The interaction of native calf thymus DNA (CT-DNA) with isatin was studied at physiological pH by spectrophotometric, spectrofluorometric, competition experiment, circular dichroism, and viscometric techniques. No red shift and isobestic points are observed in UV absorption band of isatin. A strong fluorescence quenching reaction of DNA to isatin was observed, and the binding constants (Kf) of DNA with isatin and corresponding numbers of binding sites (n) were calculated at different temperatures. Thermodynamic parameters enthalpy change (ΔH) and entropy change (ΔS) were calculated to be +27.42 kJ mol⁻¹ and +201 J mol⁻¹ K⁻¹ according to Van't Hoff's equation, which indicated that the reaction is predominantly entropically driven. DNA viscosity and iodide quenching results suggest that isatin does not intercalate into the DNA base pairs. Circular dichroism spectra of CT-DNA indicated deep conformational changes in the DNA double helix. These results indicate that isatin interacts with CT-DNA via groove binding mode.
DNA and cell biology 10/2010; 29(10):639-46. · 2.28 Impact Factor
