The snthesis and characterization of cobalt(II), nickel(II), copper(II) and zinc(II) complexes of azo ligand 4-[(5-acetyl-2-aminophenyl)- diazenyl]-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one derived from 4-aminoantipyrine and 4-aminoacetophenone are reported. The nature of the compounds have been studied followed by mole ratio and methods of continuous contrast, Beer′s law followed during a condensation rate (1 × 10-4 – 3 × 10-4 M). The analytical data showed that all the complexes are in 1:2 metal-ligand ratio. An octahedral geometry have been suggested for all the compounds and biological studies of all the complexes were evaluated against different types of antimicrobial strains.
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
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)
Many pathophysiological processes can affect the pharmacokinetic properties of drugs in people with diabetes. The present study was deigned to evaluate the influence of diabetes mellitus (DM) on the pharmacokinetic parameters of metronidazole administered as single oral dose. Twelve healthy volunteers and twelve diabetic patients were enrolled in the present study. On day 1, a single oral dose of metronidazole 500 mg was administered orally to all participants at 9:00 am after a 10-hour fasting. Over the following 48 hours, blood samples were taken at frequent intervals and serum metronidazole concentrations were measured by a high-performance liquid chromatography method for assessment of pharmacokinetics of metronidazole. The data
... Show MoreMany pathophysiological processes can affect the pharmacokinetic properties of drugs in people with diabetes. The present study was deigned to evaluate the influence of diabetes mellitus (DM) on the pharmacokinetic parameters of metronidazole administered as single oral dose. Twelve healthy volunteers and twelve diabetic patients were enrolled in the present study. On day 1, a single oral dose of metronidazole 500 mg was administered orally to all participants at 9:00 am after a 10-hour fasting. Over the following 48 hours, blood samples were taken at frequent intervals and serum metronidazole concentrations were measured by a high-performance liquid chromatography method for assessment of pharmacokinetics of metronid
... Show MoreBackground: Diabetes mellitus type 2 has been known for many years as the most common endocrine metabolic disorder that affect the oral cavity and cause many oral diseases including candidiasis. In this study, the incidence of Candida spp. in the saliva of controlled and uncontrolled diabetic patients were determined and compared with non diabetic group. Material and method: The sample consists of 200 subjects: 100 diabetic patients [57 (28.5%) uncontrolled diabetes, 43 (21.5%) controlled diabetes] and 100 (50%) non diabetic groups. Saliva samples was obtained from the subjects and cultured on selective media using appropriate microbiological method to observe the presence of Candida spp. Results: The results revealed a significant associat
... Show More Sixteen new complexes with the general formula [M(L)2(H2O)2] were prepared resulting from the reaction of the two new Schiff base ligands, which are: - L1= (E)-5-((2-hydroxybenzylidene)amino)-2-phenyl-2,4-dihydro-3H-pyrazol-3-one) L2 = (E)-5-((2-hydroxy-3-methoxybenzylidene)amino)-2-phenylpyrazolidin-3-one) With divalent metal ions (manganese, cobalt, nickel, copper, zinc, cadmium, mercury) and (tetravalent platinum). Ligands was derived from the reaction of the amine (5-amino-2-phenyl-2,4-dihydro-3H-pyrazol-3-one) with Salicylaldehyde and ortho-vanillin, which is linked to the metal ions via the nitrogen atoms are the isomethene group and the oxygen is the hydroxide group of t
... Show MoreThis review is concluded of 8-Hydroxyquinline (8HQ) compound and derivatives which has a very significant interests with a strong fluorescence , furthermore the relationship between divalent metal ions and characteristic of chelating . In the same way coordinated features have increase of its organic action and inorganic behavior by giving many samples of compounds which are a good chelating agents ligands with more capable of forming very stable complexes.Therefore, the role of (8HQ) is not limited on complexes only but its applications in different fields so this review will focus on demonstration preparation methods and properties of (8HQ) derivatives with their complexes and applications, hopefully that we will cover a part of scientifi
... Show MoreThe present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydro
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