New Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N,N'E,N,N'E)-N,N'-(cyclohexane-1,3-diylidene)bis(4- fluoro-3-(1H-tetrazol-5-yl)aniline) (L1). The reaction of these ligands with the appropriate metal ions gave polymeric metal complexes of the formulae {[M2(L)]Cl}n and [M(L1)Cl2]n (where M = Co(II), Ni(II) and Cd(II)). A range of techniques were used to confirm the entity of ligands and their complexes. The formation of ligands and mode of complexation and geometrical structure of the title polymeric complexes were verified using FTIR, electronic spectra, NMR, ESMS, magnetic susceptibility, micro-elemental analysis, metal content, chloride content and conductance. The analytical and spectroscopic data indicated the formation of four-coordinate complexes, with a tetrahedral geometry for Co(II) and Cd(II), and square planer for Ni(II) in L- and L1 complexes. Biological evaluation of ligands and their polymeric complexes against gram-positive bacteria (G+), Bacillus stubtili, Staphylococcus aureus, and gram-negative bacteria (G−), Escherichia coli and Pseudomonas aeruginosa, showed ligands and their polymeric metal complexes have a good effect on the screened bacteria.
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting
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Certain cyclic amine derivatives of metronidazole via acetate spacer were prepared. Cyclic amines used are piperidine and piperazine to improve the physicochemical properties and reduce some of metronidazole side effects. This is believed to be done by modification of its structural features to get prodrugs with improved properties over that of metronidazole. The present work includes esterification of metronidazole with choroacetic acid, N-alkylation of the cyclic amines by the halogenated ester and characterization of their structures by spectral(UV and IR) and elemental(CHN)analysis.The melting points, degree of solubilities and partition coefficients were also determined. Both metronid
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A Photo Dynamic Therapy (PDT) is a technique which is used with Laser to treat many of cancer
tissues. This paper deals with the relatively new therapeutic technique (PDT) with pulsed Nd:glass Laser
which was applied to human soft tissues (Ovary and Kidney tissues), and to the hard tissues (freshly
extracted human teeth), with power density of 280 watt/mm2 and exposure time 330 usec. Different
dyes (Blue, methylene, eosin, and orange) were applied to the area before irradiation to study the effect
of the pigments on the laser interaction with biological tissues. The zone of treatment (Z-necrosis) with
aid of MATLAB was determined. The relationship of zone of treatment with exposure time,
accumulated damage and fracti
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The present work involved designing and synthesizing of a series of new. compounds which their molecules are composed from two biologically active components namely sulfamethoxazole or β-lactam containing drugs and cyclic imides. The target new compounds were synthesized by two steps in the first one a series of six bis (N-drug phthalamic acid_4-yl) ketone (1-6) were prepared from the reaction of sulfamethoxazole or β-lactam containing drugs with benzophenone 3, 3′, 4, 4′ -tetracarboxylic dianhydride.
In the second step, compounds (1-6) were introduced in dehydration reaction via fusion process producing the target compounds bis (N-drug phthalimidyl-4-yl) ketone (7-12). The antibacterial and antifungal high
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A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of di
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A simple, economical and selective method employing ion pair dispersive liquid−liquid microextraction (DLLME) coupled with spectrophotometric determination of carbamazepine (CBZ) in pharmaceutical preparations and biological samples was developed. The method is based on reduction of Mo(VI) to Mo(V) using a combination of ammonium thiocyanate and ascorbic acid in acidic medium to form a red binary Mo(V) thiocyanate complex. After addition of CBZ to the complex, extraction of the formed CBZ−Mo(V)−(SCN)6 was performed using a mixture of methylene chloride and methanol. Then, the measurement of target complex was performed at the wavelength of 470 nm. The important extraction parameters affecting the efficiency of DLLME were studied and o
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Reaction of L1 [((E)-N1-(nitrobenzylidene)benzene-1,2-diamine] and L2( m-aminophenol), and one equivalent of di- or tri-valent metals(Cr(ӀӀӀ), Mn(ӀӀ), Fe(ӀӀӀ), Co(ӀӀ), Ni(ӀӀ), Cu(ӀӀ) and Zn(ӀӀ) afforded the complexes [M(L1)(L2)2]Cl, M=Cr(ӀӀӀ) and Fe(ӀӀӀ) and the complexes [M(L1)(L2)2] M= Mn(ӀӀ), Co(ӀӀ), Ni(ӀӀ), Cu(ӀӀ) and Zn(ӀӀ). The structure of the Schiff base ligand and their complexes are characterized by (C:H:N), FT.IR, UV.Vis, 1HNMR, 13CNMR and mass spectral. The presence of metal in the complexes are characterized by flame atomic absorption. The spectral data of the complexes have revealed the octahedral geometry. The (L1), (L2) and mixed ligand metal complexes were screened for their ability as cataly
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