Eighteen new cyclic imides (maleimides) conncted to benzothiazole moiety through sulfonamide group were synthesized via multistep synthesis.The first step involved preparation of two maleamic acids N-phenylmaleamic acid and N-benzylmaleamic acid via reaction of maleic anhydride with aniline or benzyl amine.Dehydration of the prepared amic acids by treatment with acetic anhydride and anhydrous sodium acetate in the second step afforded N-phenylmaleimide and N- benzyl maleimide which in turn were treated with chlorosulfonic acid in the third step to afford 4-(N-maleimidyl) phenyl sulfonyl chloride and 4-(N-maleimidyl) benzyl sulfonyl chloride respectively.In the Fourth step of this work each one of the two prepared maleimidyl sulfonyl chlorides was introduced in reaction with nine substituted-2-amino benzothiazole compounds producing nine N-(4-(N-substituted benzothiazole -2-yl) sulfonamido phenyl) maleimides and nine N-(4-(N-substituted benzothiazole-2-yl)snlfonamido benzyl) maleimides.More over another new six sulfonamide phenyl and benzyl maleimides substituted with other heterocycles (pyridine and phenazone )were prepared via reaction of 4-(N-maleimidyl) phenyl and benzyl sulfonyl chlorides with heterocyclic amines including (2-amino pyridine,4-amino-pyridine,4-aminophenazone). Microbiological activity of the prepared compounds against two typs of bacteria(staphylococcus aureus and klebsiella pneumonia) and (candida albicans) fungi were evaluated and the results showed that these compounds have good antibacterial and good antifungal activities.
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
Anaerobic digestion (AD) is the most common process for dealing with primary and secondary wastewater sludge. In the present work, four pre-treatment methods (ultrasonic, chemical, thermal, and thermo-chemical) are investigated in Al-Rustumya Wastewater Treatment plant in order to find their effect on biogas production and volatile solid removal efficiency during anaerobic digestion.
Two frequencies of ultrasonic wave were used 30 KHz and 50 KHz during the pre-treatment. Sodium hydroxide was added in different amounts to give three pH values of 9, 10 and 11 in chemical pre-treating processes. The sludge was heated at 60oC and 80oC through thermal pre-treatment experiment. Also, the sludge was treated thermo-chemically at 80 oC and pH
The study was aimed to determine the coordinates of the points were measured by different ways and different instruments, the most precise way using the differential global positioning system (DGPS) that will be the reference measurements in comparison, less precise way using navigator GPS. Google earth (pro.), and the other applications of GPS mobile ( Samsung and I-phone). In this research (8 points) were chosen that are occasional in location. The comparison of the different observations can give us an idea of the extent to which the accuracy of the observations differs from the different devices used in the observing, as well as through the knowledge of the best device and the best way to measure coordinates accurately t
... Show MoreThis investigation showed (31) species belonging to (15) genera under (five) families and two orders. The leafminers Dipter families (Agromozidae, Anthomyiidae, Drosophilidae), Agromyzid flies is the highest level of investigated many host plants, but other families have lowest host plants. The synonyms of species were provided from GBIF scarlet's. The date and localities of sampling collection were recorded.
It is found that hypersensitive teeth have a larger number and wider patent tubules than those of non-sensitive teeth. Objective: The aim of this study is to compare between the effects of diode laser at different power densities, with and without sodium fluoride on the sealing of exposed dentinal tubules and dentin permeability. Materials and methods: 118 teeth were used. Samples were divided into three major groups. The first consisted of 100 teeth used for permeability test. The second consisted of 16 teeth for measuring external surface temperature elevation while irradiation. The third, in turn, consisted of one pair of teeth observed under SEM for dentine surface morphology analysis. Results: For dentin permeability measurement, th
... Show MoreNew series of 4, 4'-((2-(Aryl)-1H-benzo [d] imidazole-1, 3 (2H)-diyl) bis (methylene)) Diphenol (3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr
... Show MoreNew series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hy
... Show MoreBackground: ;Hepatitis C virus (HCV) is a major cause of chronic liver disease. Approximately 85% of patients acutely infected with HCV progress to chronic liver disease with persistence of HCV-RNA for more than 6 months Among patients with chronic HCV infection , 15-20% progress to end-stage liver disease main transmission methods of the virus is by : blood and blood products ; sharing needles and acupuncture .Objective: To evaluate Iraqi patients infected with chronic HCV, including their treatment, and factors that affect their response to treatment .Methods :This study was performed at Gastroenterology and Hepatology hospital in Baghdad from January 2011 to March 2012.The study enrolled 90 patients with HCV Antibody positive (Ab +ve)
... Show MoreThe prospective study has been designed to determine some biomarkers in Iraqi female patients with
breast cancer. The current study contained 30 patients whose tissue samples have been collected from
hospitals in Medical City in Baghdad after consent patients themselves and used immunohistochemical
technique to determine these markers. The results showed a significant correlation between ER and PR tissue
markers (Sig = 0.000) and a significant correlation between cyclin E phenotype and cyclin E intensity (Sig =
0.001).