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.
Abstract
The experiment has been carried out in the Syrian National Commission of Biotechnology, during the growing season 2018/2019, to study the effect of abiotic stresses (salinity and osmotic stresses) on the activity of some antioxidant enzymes and biochemical traits in Catharanthus roseus. The experiment has been laid according to (CRD) with three replications. The seeds have been sterilized by NaOCl solution (0.5% v/v), then planted on MS medium. Plantlets have been moved to MS medium enriched with NAA (1 mg.L-1) and BA (2 mg.L-1). The callus has been initiated from leaves using MS medium containing NAA (1 mg L-1) and KIN (2 mg.L-1). After 60 days, callus
... Show MoreThe paper presents an original method to make the geometric synthesis of the rotary cam and translated tappet with roll. Classical method uses to the geometric synthesis and the reduced tappet velocity, and in this mode the geometric classic method become a geometric and kinematic synthesis method. The new geometric synthesis method uses just the geometric parameters (without velocities), but one utilizes and a condition to realize at the tapped the velocities predicted by the tapped movement laws imposed by the cam profile. Then, it makes the dynamic analyze for the imposed cam profile, and one modify the cam profile geometric parameters to determine a good dynamic response (functionality). In this mode it realizes the dynamic synthesis
... Show MoreThis study examines the dynamic relationship between stock market and economic activity in the United States to verify the possibility of using financial indicators to monitor the turning points in the expected path of future economic activity. Has been used methodology (Johansen - Juselius) for the Co-integration and causal (Granger) to test the relationship between the (S & P 500 , DJ) index and gross domestic product (GDP) in the United States for the period
(1960-2009). The results of the analysis revealed the existence of a causal relationship duplex (two-way) between the variables mentioned. which means the possibility of the use stock market indicators to pre
This study is conducted to evaluate the therapeutic and antioxidant effect of lemon juice on some hematological and biochemical parameters. Thirty female mice used in this study were exposed to oxidative stress through giving them hydrogen peroxide in drinking water for 30 days. Animals randomly distributed over 3 groups, each group contained 10 animals and treated as follows: T1 control group (drinking distilled water only), T2 (0.75% hydrogen peroxide in drinking water) and T3 (0.75% hydrogen peroxide in drinking water with daily drenching with 1 mL lemon juice). At the end of the experiment, blood samples were collected from animals for evaluating the following hematological and biochemical parameters: Haemoglobin concentration (Hb),
... Show More: Partial purification of phosphoenolpyruvate carboxykinase (PEPCK) from type 2 diabetic patients sera take place using some purification steps such as participation with ammonium sulphate (55-80%) and filtered through dialysis, then ion exchange chromatography by DEAE sepharose anion column, gel filtration chromatography by sephadex G-100 column. In ion exchange step, there are four peak are obtained, the highest enzyme activity obtained by (0.4 M Nacl) with purification fold (2.18), yield (44.3) of enzyme and specific activity (13.5) mg/ng, which obtained a single peak by gel filtration chromatography, the degree of purification (5.34) fold, yield of enzyme (20%) with specific activity (33.109mg/ng). The purified enzyme had an optimum tem
... Show MoreBismuth oxide nanoparticle Bi2O3NPs has a wide range of applications and less adverse effects than conventional radio sensitizers. In this work, Bi2O3NPs (D1, D2) were successfully synthesized by using the biosynthesis method with varying bismuth salts, bismuth sulfate Bi2(SO4)3 (D1) or bismuth nitrate. Penta hydrate Bi(NO3)3.5H2O (D2) with NaOH with beta-vulgaris extract. The Bi2O3NPs properties were characterized by different spectroscopic methods to determine Bi2O3NPs structure, nature of bonds, size of nanoparticle, element phase, presence, crystallinity and morphology. The existence of the Bi2O3 band was verified by the FT-IR. The Bi2O3 NPs revealed an absorption peak in the UV-visible spectrum, with energy gap Eg = 3.80eV. The X-ray p
... Show MoreThe study aimed to purification of acid phosphatase (ACP) from sera of obesetype 2 diabetes mellitus patients, this study included from thirty T2DM patients and thirty control, purification process was done with several steps included precipitation with inorganic salt (NH4 ) 2SO4 30%-80%, dialysis, ion exchange chromatography by DEAE sepharose anion column and size exclusion chromatography by Sepharose 6B.ACP, BMI, FBS, HbA1c, Lipid profile, Urea, Creatinie, Insuline, Homa-IR were determined. Results showed the precipitate and concentrated protein appeared four peaks in ion exchange column. ACP located in the first and second peak with purification fold (21.1), (37.2) yield of enzyme and specific activity (173.3) IU/ml, which obtained a si
... Show MoreObjective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreObjective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreBackground: Verrucous carcinoma (VSCC) is considered as a rare well differentiated carcinoma variant of SCC with no metastatic potential. The aim of this study is to evaluate the Immunohistochemical expression MMP-2, VEGF and D2-40 expression in OSCC and VSCC. Materials and methods: Thirty formalin fixed paraffin embedded tissue blocks of OSCC and another twelve VSCC were collected and Four micrometer thick sections were cut from each block and mounted on positively charged slides and stained immunohistochemically with monoclonal antibodies to MMP-2, VEGF and D2-40. Results: there is no statistical difference between SCC and VSCC regarding the immunoexpression of MMP-2 and VEGF. While the lymphatic vessels density were higher in SCC than V
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