The work involves synthesis of new Schiff bases ([V] a, b and [VI] a, b), pyrazoles [VII] a, b and pyrazolines [VIII] a, b derivatives containing isoxazoline unit starting with chalcones. 4-bromoacetophenone was reacted with 4-hydroxybenzaldehyde or 4-hydroxyacetophenone was reacted with 4-bromobenzaldehyde in basic medium to give chalcone by Claisen-Schemidt reaction. The chalcons [I] a, b was reacted with hydroxylamine hydrochloride to form isoxazolines [II] a, b. which were reacted with ethyl chloro acetate in basic medium to get ester compounds [III] a, b. The condensation new ester [III] a, b with hydrazine hydrate80% yieldedacid hydrazide [IV] a, b. The later compound refluxing with 4-substituted benzaldehyde in dry benzene to give Schiff bases ([V] a, band [VI] a, b) while the reaction of acid hydrazide [IV] a, b with acetylacetone or ethyl aceto acetate to get pyrazole [VII] a, b, pyrazolone [VIII] a, b, respectively. The synthesized compounds were characterized by melting points, FTIR, mass and 1H NMR spectroscopy
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)
This experiment examined the effects of adding sodium alginate and Kojic acid as substitutes for conventional antibiotics to Skim milk extender on the characteristics of cryopreserved and frozen buffalo bull semen, as well as the evaluation of their additions as antibiotics that help lower the microbial load. Following the collection and dilution of the Skim milk extender, the experimental treatments were separated into five groups, as follows: T1: (control-) without adding any antibiotics; T2: (control+) adding the conventional antibiotics Gentamicin 0.4 IU and Tylosin 0.08 IU per 100 ml; T3: adding Kojic acid at (0.06 g/L) T4: adding sodium alginate at (0.6 mg/mL)T5: adding a combin
This experiment was conducted to evaluate the effect of foliar spraying with gibberellic acid concentrations (0,50,100)mg.L¹ and proline acid concentrations (0, 25, 50)mg.L¹ and their interactions on some growth parameters of pea plant using clay pots in the botanical garden of Biology Department College of Education for pure science Ibn –Al-Haitham ,Baghdad University, for the growing season 2012-2013 the experiment involved the studing of some growth parameters as plant?s height, dry weight, wt. of pods.plant¹, biology yield and the concentration of some major elements (nitrogen, phosphorus and calcium) in plant?s seeds. The experiment was designed according to Completely Randomized Desig(CRD) with three replications. R
... Show MoreIn this paper, two new simple, fast and efficient block matching algorithms are introduced, both methods begins blocks matching process from the image center block and moves across the blocks toward image boundaries. With each block, its motion vector is initialized using linear prediction that depending on the motion vectors of its neighbor blocks that are already scanned and their motion vectors are assessed. Also, a hybrid mechanism is introduced, it depends on mixing the proposed two predictive mechanisms with Exhaustive Search (ES) mechanism in order to gain matching accuracy near or similar to ES but with Search Time ST less than 80% of the ES. Also, it offers more control capability to reduce the search errors. The experimental tests
... Show Moreالخلاصة لقد شكل المحافظون الجدد وهم بالأساس نخبة من المثقفين ومن السياسيين الأمريكيين كتلة ضغط كبيرة التأثير على الإدارة في عهد الجمهوريين. حمل هؤلاء المحافظون مشروعاً إيديولوجياً البسوه لسلطة الجمهوريين وهو يهدف إلى جعل أمريكا سيدة العالم من دون منازع خاصة بعد انهيار الاتحاد السوفييتي ونهاية الحرب الباردة. واكب هذا الحدث التاريخي الكثير من الأفكار ومنها (نهاية التاريخ)، وصراع الحضارات، وكذ
... Show MoreA comparison study was made for the reaction of triruthenium carbonyl Ru3(CO)12 with azoarene ArN=NAr . This reaction was monitored in two kinds of solvents , toluene , and n- octane , which yielded new triruthenium carbonyl complex Ru3(μ3-NAr)2(CO)9 . The reactions of azoarenes ArN=NAr with Ru3(CO)12 formed the following trinuclear compound of Ru3((μ3- NAr)2(CO)9 (Ar-C6H4Br-4) in law yield . In addition , to new isomers species of mononuclear cyclometallated of Ru(BrC6H4N-NC6H4NBr-4)2(CO)2 in different percentages . The mechanism of the reaction domenstrates that the formation of trinuclear bis arylimido complexes , and ortho metallated was , the result of cleavage of nitrogen –nitrogen bond . Monitoring this gave evidence that the rea
... Show MoreFatty Acid Methyl Ester (FAME) produced from biomass offers several advantages such as renewability and sustainability. The typical production process of FAME is accompanied by various impurities such as alcohol, soap, glycerol, and the spent catalyst. Therefore, the most challenging part of the FAME production is the purification process. In this work, a novel application of bulk liquid membrane (BLM) developed from conventional solvent extraction methods was investigated for the removal of glycerol from FAME. The extraction and stripping processes are combined into a single system, allowing for simultaneous solvent recovery whereby low-cost quaternary ammonium salt-glycerol-based deep eutectic solvent (DES) is used as the membrane phase.
... Show MoreSecnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 1
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