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)
An inert matrix that is used to control the release of (PTX) was prepared using Eudragit RL100 and RSPM types as matrix forming agent . The matrices were prepared by either dry granulation(slugging) , or wet granulation method using chloroform as a solvent evaporation vehichle. The cumulative release was adjusted by using polyvinylpyrollidone (PVP) or ethylcellulose (EC) polymers .The results indicated that both methods of preparation were valid for incorporation PTX as a sustained release granules .Moreover ,the results revealed that best polymer used was Eudragit RSPM in 3:20 polymer drug ratio .Besides to that , the results indicated that the release profiles were affected by pH- medium&
... Show MoreAll new compounds synthesized by many reactions starting from a product the compounds [I]a,b from reaction of 3-phenylenediamine or 4-phenylenediamine with chloroacetyl chloride, then the compounds [I]a,b reacted with potassium thiocyanate to yield compounds [II]a,b. While the compounds[III]a,b yield from reacted the compounds [I]a,b with sodium azide then the compounds [III]a,b reacted 1,3-dipolar cycloaddition reaction with acrylic acid to give compounds [IV]a,b and the later compounds reacted with phenylene diamine to product benzimidazole compounds [V]a,b . In addition to synthesized acid chloride compounds [VI]a,b by reacted the compounds [IV]a,b with thionyl chloride .Finally reacted the compounds [VI]a,b with different aromatic amine
... Show MoreEleven new 2,6-di-tert-butyl-4-(5-aryl-1,3,4-oxadiazol-2-yl)phenols 5a–k were synthesized by reacting aryl hydrazides with 3,5-di-tert butyl 4-hydroxybenzoic acid in the presence of phosphorus oxychloride. The resulting compounds were characterized based on their IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the compounds. Compounds 5f and 5j exhibited significant free-radical scavenging ability in both assays.
A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct
... Show MoreObjective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid,
... Show Moreتعد لعبة كرة السلة من الألعاب الرياضية التي تحتاج متطلبات بدنية ووظيفية خاصة بها، وذلك من خلال الانتقال داخل الملعب بالكرة أو بدونها والسبل للتخلص من ملاحقة الخصم أثناء الدفاع وكيفية المناورة أثناء الهجوم مع إجادة التصويب بكافة أنواعه داخل الملعب، ومن هنا تكونت مشكلة البحث في كيفية تطوير تلك العوامل الوظيفية والتي لها الأثر في الارتقاء بمستوى أداء اللاعب أثناء اللعب، وعن طريق استخدام الباحثان لطريقة جهاز ا
... Show MoreGold nanoparticles AuNPs have proven to be powerful tools in various nanomedicine applications, because of their photo-optical distinctiveness and biocompatibility. Noble metal gold nanoparticles was prepared by pulsed laser ablation method (1064-Nd: YAG with various Laser power from 200 to 800 mJ and 1 Hz frequency) in distil water. The process was characterized using UV-VIS absorption spectroscopy. Morphology and average size of nanoparticles were estimated using AFM and X-ray diffraction (XRD) analysis which show the nature of gold nanoparticles (AuNPs). Antibacterial activity of gold nanoparticles as a function of particles concentration against gram negative bacterium Escherichia coli and gram positive bacterial Staphylococcus aureu
... Show MoreMultiple sclerosis (MS) is a chronic, inflammatory demyelinating disease of central nervous system with complex etiopathogenesis that impacts young adults (Lee et al., 2015), and MS impacts younger and middle aged character and leads to a range of disabilities that can alter their daily routines (Yara et al, 2010). Although, the exact cause of MS is still undetermined, the disease is mediated by adaptive immunity through the infiltration of T cells into the central nervous system (Bjelobaba et al, 2017). MS causes the Focal neurological symptomsand biochemical changes in the molecular level and the variation of neural cells such as loss or alteration of sensation, motor function, visible signs such as blurred vision or transient blindness,
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