ABSTRACT
Oxazepam and lorazepam inhibit the adenosine deaminase (ADA) differently. In the case of lorazepam temperature increment causes an increase in the inhibition potency whereas higher temperature reduces the inhibitory effect of oxazepam; which proposes the overall profounder structural changes in the case of lorazepam relative to those caused by oxazepam.
Subject(s)
Adenosine Deaminase/chemistry , Adenosine Deaminase/metabolism , Enzyme Inhibitors/metabolism , Lorazepam/metabolism , Oxazepam/metabolism , Adenosine/metabolism , Adenosine Deaminase Inhibitors , Animals , Anti-Anxiety Agents/metabolism , Anticonvulsants/metabolism , Cattle , Circular Dichroism , Computer Simulation , Hypnotics and Sedatives/metabolism , Intestinal Mucosa/enzymology , Kinetics , Ligands , Models, Molecular , Protein Conformation , Spectrometry, Fluorescence , Structure-Activity Relationship , TemperatureABSTRACT
A novel coated wire electrode (CWE) for Al(III) ions is described based on 2-(1H-benzo[d]imidazole-1-yl)-1-phenylethanoneoxime as a new ionophore in carbon-PVC composite. The sensor exhibits significantly enhanced selectivity toward Al(3+) ions over the concentration range 4.3 x 10(-7) to 5.0 x 10(-2)M with a lower detection limit of 2.5 x 10(-7) M and a Nernstian slope of 19.41+/-0.52 mV decade(-1) of aluminium activity. This sensor has a short response time of about 10s and is reproducible and stable for at least forty-five days. This proposed CWE which is designed for the first time revealed good selectivity for Al(III) over a wide variety of other cations. The performance of the sensor is best in the pH range of 3.1-5.5 and it also works well in partially non-aqueous medium. Moreover, the assembly has been successfully used as an indicator electrode in the potentiometric titration of aluminium (III) against EDTA and also in determining Al(III) quantitatively in pharmaceutical and mineral water samples.
Subject(s)
Aluminum/analysis , Carbon/chemistry , Mineral Waters/analysis , Pharmaceutical Preparations/chemistry , Platinum/chemistry , Electrodes , Hydrogen-Ion Concentration , Surface PropertiesABSTRACT
In this investigation, the effects of synthesized 4-chloro-2,6-bis-(2-hydroxyl-benzyl)-phenol (CBHBP) on cutaneous wound healing and growth of some of the wound contaminating microorganisms were studied. The antibacterial effects of this compound were then evaluated on Staphylococcus aureus (S. aureus), Pseudomonas aeruginosa (P. aeruginosa), Escherichia coli (E. coli) and Klebsiella spp., using solid dilution method. It was demonstrated that CBHBP has a significant antimicrobial activity against S. aureus but it is not effective in the case of other microorganisms studied in this experiment. The effect of local administration of CBHBP on healing of a standard full-thickness 2 cm skin incision of skeletally mature rats was evaluated. Histological changes together with mechanical properties and dry weight content of the healing tissues at the site of the lesions were assessed in treated and untreated animals. It was observed that the injured area of the treated animals was more organized and showed more fibroblasts and less inflammatory cells. Much better maturation criteria in treated tissues were observed in comparison with those of the untreated ones which contained numerous polymorphonuclear inflammatory cells after 14 days post-injury. Many infiltrated macrophages and lymphocytes were present even 28 days after injury induction in the haphazardly organized dermis and also in subcutaneous tissues of the untreated animals. The percentage dry weight content of the treated lesions at 14 days post-injury was remarkably higher than those of the untreated animals. The results of biomechanical tensile testing showed that the ultimate tensile strength and stress of the injured skin of the treated animals were higher than those of the untreated ones. From these results, it could be concluded that CBHBP can be effective on wound healing and may be considered as a treatment regimen after evaluating its mechanism of action as well as testing its contraindications.
Subject(s)
Anti-Infective Agents, Local/pharmacology , Chlorophenols/pharmacology , Wound Healing/drug effects , Wound Infection/drug therapy , Wounds and Injuries/drug therapy , Animals , Colony Count, Microbial , Disease Models, Animal , Dose-Response Relationship, Drug , Escherichia coli/drug effects , Klebsiella/drug effects , Male , Microbial Sensitivity Tests , Pseudomonas aeruginosa/drug effects , Random Allocation , Rats , Skin/injuries , Skin/microbiology , Staphylococcus aureus/drug effects , Treatment Outcome , Wounds and Injuries/microbiologyABSTRACT
In view of obtaining some potential antibacterial compounds, we have described synthesis of some chloroaryloxyalkyl imidazole and benzimidazole derivatives. The relevant step in the synthetic sequence was the initial condensation of 4-chloro or 2,4-dichlorophenol with 1, n-dibromoalkanes (n=2, 4, 5) to provide compounds 3a-f in sufficient yields. The subsequent condensation of 3a-f with some imidazole derivatives and benzimidazole afforded products 4a-l and 5a-e in good yields. Some of compounds 4a-l as well as 5a-e were tested in vitro against Salmonella typhi O-901 and Staphylococcus aureus A 15091. Compounds 4a and 4c showed considerable bactericidal activities against tested bacteria. Compound 4b showed significant activity against S. aureus A 15091 but was inactive against S. typhi O-901. Other compounds showed intermediate activities against S. aureus A 15091 but most of them were inactive against S. typhi O-901. Semiempirical AM1 calculations showed that negative electrostatic potentials around oxygen of the phenoxy and nitrogen of the imidazole moieties have direct effect on the antibacterial activity towards S. aureus A 15091. In QSAR analysis, different electronic, topologic, functional groups and physicochemical descriptors were calculated for each molecule and a three parametric equation was found between the logMIC and HOMO energy, hydration energy and number of primary carbon atoms of the molecules.
