Search

[Display omitted] • VO2+- and MoO 2 2+-complexes of tratrato-dihydrazone derivative are synthesized and characterized. • The antimicrobial (bacteria and fungi) and anticancer potential of VO2+- and MoO 2 2+-complexes and their ligand are examined. • Their binding to ct DNA is examined via UV–Visible spectroscopy and hydrodynamic measurements. • VO2+- and MoO 2 2+-complexes exhibited more biological reactivity over their free ligand based on Tweedy's chelation theory. Form the condensed > C = O of salicyldehyde with -NH 2 of tartric dihydrazide, a new chelating bis -tridentate tartrato-dihydrazone ligand (HTL) was constructed. Due to the high applicability of metal aryl/aroyl-hydrazone complexes, its ligational behavior versus two high valent dioxo/oxo-metal ions of MoO 2 2+ and VO2+ ions was explored to build up two new organo-dimetallic complexes (MoO 2 TL and VOTL, respectively). Chemical structure elucidation of HTL, MoO 2 TL, and VOTL was formulated through the analyses of different spectroscopic tools, along with the thermogravimetric and micro-elemental analyses, the conductance and magnetic measurements. The inhibition strength of the current compounds against the growth of various entitled microorganisms and tumor cell lines of humans was evaluated regarding the role action of the high valent metal ions (MoO 2 2+ and VO2+ ions in their metallodrug candidates). Both MoO 2 TL and VOTL displayed a significant inhibition action more than that of HTL based on the inhibition zone areas in mm for the microbial series and the half inhibitory concentration in µM (IC 50) for the tumor cell lines of their cells' growth. Also, the interactive and binding nature of HTL, MoO 2 TL, and VOTL with calf thymus DNA (ct DNA) was evaluated viscometric and spectrophotometric titrations. The interactive modes of HTL, MoO 2 TL, and VOTL was estimated within the chromism type, the Gibb's free energy, and binding constant values (Δ G b ≠ and K b , respectively), with reported magnitudes Δ G b ≠ (Gibb's free energy) = -42.06, −48.11 and −47.67 kJ mol−1, and K b (binding constant) = 14.09, 17.11 and 16.89 × 107 mol−1 dm3, respectively. The bio-reactivity of both MoO 2 TL and VOTL complexes was modified compared to that of HTL towards ct DNA with covalent/non-covalent and replacement binding interaction. [ABSTRACT FROM AUTHOR]

New series of oxo-vanadium N -salicyledieneamino acid Schiff base complexes are synthesized and characterized. They are synthesized from the reaction of sodium salicylaldehyde-5-sulfonate, some amino acids, alanine (VOHL1), leucine (VOHL2) or glycine (VOHL3) in an aqueous media, and leucine (VOHLpy1) or tryptophan (VOHLpy2) in pyridine with vanadyl acetylacetonate. The complexes are characterized by EA, TGA, IR, UV–Visible and mass spectra, conductivity and magnetic measurements. The biological activity of the VO-complexes shows that VOHL1, VOHL2 and VOHL3 exhibit anti-proliferative effect and may be used as anticancer drugs. VO-complexes manifest high toxicity, except VOHL2 is less toxic, and could be applied for the human being. VOHL1, VOHL2 and VOHL3 display remarkable SOD like potential and act as high inhibiting reagents. VOHLpy1 and VOHLpy2 show low inhibiting potentials. VO-complexes have good anti-oxidant effect, in which VOHL3 affords the best antioxidant activity. The interaction between VO-complexes and DNA is studied spectrophotometrically and by gel electrophoresis. Binding constants and spectrophotometric parameters indicate a strong interaction between VO-complexes and DNA. VO-complexes have respectable anti–bacterial and antifungal activities, where VOHL3 shows the maximum potential. DFT calculations of VOHL1 and VOHL3 were discussed in the light of their biological activity, which are convenient with the obtained results. [ABSTRACT FROM AUTHOR]

• A new set of hydronaphthalene-sulfonamides were synthesized in a facile approach. • Some of the synthesized agents reveal potent antimicrobial properties. • The promising candidates showed high level of safety towards the human normal cells. • 2D-QSAR model described the antimicrobial properties observed. In the present work, authors successfully prepared potent antimicrobial agents of new tetrahydronaphthalene-sulfonamide derivatives, derived from new easily synthetic route of 3-methoxy-8-oxo-5,6,7,8-tetrahydronaphthalene-2-sulfonyl chloride 2. Preparation method of this compound has not been published yet, however it is available commercially expensively, which motivated us to innovate new efficient and facile method for its preparation. All the synthesized compounds were tested for in vitro antimicrobial inhibitory activities against a panel of Gram-positive, Gram-negative bacterial pathological strains and Candida Albicans. Compound 2 showed poor activity towards all of the tested pathogenic strains, but it is easily modified and converted from biologically inactive compound to highly active sulfonamide products 5a-f , or moderately active compounds 3a-k. Cytotoxic evaluation of the promising candidates 5d and 5e showed marked safety profile towards the human normal cells. QSAR study for the new compounds was carried out and was compatible with the antimicrobial results. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract: With the purpose of evaluating the ability of Pd(II) complex to interact with DNA molecule as the main biological target, two new complexes [Pd(bpy)(OH2)2] (1) and [Pd(Phenpip)(OH2)2] (2), where (bpy=2,2′-bipyridine; Phenpip=1-phenylpiperazine), have been synthesized and the binding properties of these complexes with CT-DNA were investigated. The intrinsic binding constants (K b) calculated from UV–Vis absorption studies were 3.78×103 M−1 and 4.14×103 M−1 for complexes 1 and 2 respectively. Thermal denaturation has been systematically studied by spectrophotometric method and the calculated ΔT m was nearly 5°C for each complex. All the results suggest an electrostatic and/or groove binding mode for the interaction between the complexes and CT-DNA. The redox behavior of the two complexes in the absence and in the presence of calf thymus DNA has been investigated by cyclic voltammetry. The cyclic voltammogram exhibits one quasi-reversible redox wave. The change in E 1/2, ΔE p and I pc/I pa supports that the two complexes exhibit strong binding to calf thymus DNA. Further insight into the binding of complexes with CT-DNA has been made by gel electrophoresis, where the binding of complexes is confirmed through decreasing the intensity of DNA bands. The two complexes have been screened for their antimicrobial activities using the disc diffusion method against some selected Gram-positive and Gram-negative bacteria. The activity data showed that both complexes were more active against Gram-negative than Gram-positive bacteria. It may be concluded that the antimicrobial activity of the compounds is related to cell wall structure of bacteria. [Copyright &y& Elsevier]

Abstract: The Pyrrole derivatives Ia–d were prepared and utilized for the preparation of pyrrolo[2,3-d]pyrimidine derivatives IIa–c, III, IVa–e, V and VIIIa–c; pyrrolo[3,2-e]tetrazolo[1,5-c]pyrimidine VI and pyrrolo[4,3e][1,2,4]triazolo[1,5-c]pyrimidine derivative derivatives VIIa–c. These some newly synthesized compounds were examined for their in vitro antimicrobial activity and in vivo anti-inflammatory. Result indicated that these compounds showed promising anti-inflammatory activity in comparison to ibuprofen (the standard anti-inflammatory drug). The structure–activity relationships (SAR) and anti-inflammatory activities of these compounds are also discussed in this paper. [Copyright &y& Elsevier]

Abstract: The pyrroles Ia–c were used as precursor for the preparation of pyrrolo [2, 3-d] pyrimidine-2 and/or 4 thione derivatives IIa–f. A series of 8-Aryl-pyrrolo [2, 3-d] thiazolo[3,2-a]pyrimidine VI and VII were prepared. Alkylation of the thione compounds in basic medium afforded the pyrrolo [2, 3-d] pyrimidine IV. Also, some 2-amino pyrrolo [2, 3-d]pyrimidines V were obtained. Some newly synthesized compounds were examined for their in vitro anti-inflammatory. Also, all new compounds were examined for their in vivo anti-microbial activity. Several derivatives, showed a promising anti-inflammatory activity in compared to ibuprofen. In this paper, we examine and discuss the structure–activity relationships and anti-inflammatory activities of these compounds. [Copyright &y& Elsevier]