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)
New 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 MoreProverbs and preaching Sermons in Pre-Islamic Poetry and their indications Peacefulness
تسعى المحاسبة الى مسايرة القفزات الهائلة والمتسارعة في تطور العلوم الصرفة والتطبيقية والتقدم التكنولوجي، والتي ادت على ظهور مفاهيم جديدة الغت مسلمات وبديهيات كانت سائدة لمدة طويلة، فعلى سبيل المثال: كان مخزون المواد الاولية والبضاعة التامة في المؤسسات الصناعية او التجارية يشكل العمود الفقري لها بتكاليفه ومشاكله، حتى اذا ما جاء نظام (JIT) الغى بتطبيقاته هذه المفاهيم واعتمد م
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Praise be to God, Lord of the Worlds, and prayers and peace be upon the Master of the Messengers, Muhammad, and upon all his family and companions.
The circle of taboos in the Jewish Sharia is wider than other laws, as the Jews have severe and very complicated rituals in the matter of food, which may not be found among other people of other religions, as the dietary laws that specify foods and drinks forbidden in the Jewish Sharia include very diverse topics. The Torah specified all these laws with several texts
Actinomycetes are free, spore-forming, high (G+C) ratio (>55%) saprophytic microorganisms that are widely distributed in most soils, colonize plants, and are prevalent in water. This is frequently accompanied by the production of filament airborne mycelium. Actinomycetes are well-known microcolonies for creating antibiotics and other critical bioactive components that are beneficial to humans. Approximately 70% to 80% of commercially available medications and antiviral active compounds have been synthesized so far. Secondary metabolites produced by microbes have the potential to be used in a variety of sectors, including antimicrobial agents, enzyme technology, pigment manufacture, antitumor agents against cancer cells, and toxin pr
... Show MoreThe Sultanate of Oman is located in the far southwest of the Arabian Peninsula and enjoys a distinctive geographical location as it overlooks the Arabian Gulf and the Gulf of Oman. The Sultanate has good relations with various countries of the world and enjoys an important regional position. At the beginning of 2020, Sultan Qaboos bin Said died, and Haitham bin Tariq assumed power after him, according to the will of his cousin, the late Sultan. The new Sultan had held some important positions before 2020, including: Minister of Heritage and Culture since February 2002, Chairman of the Supreme Committee for the Future Vision (Oman 2040), Secretary-General of the Ministry of Foreign Affairs, Undersecretary of the Ministry of Foreign Affairs f
... Show MoreIn the present study, a novel ligand (L) made of 2-hydroxynaphthaldehyde and 3-hydrazone-1,3-dihydro-indole-2-one(3-[(3-hydroxynaphthalen-2-yl-ethylidene)-hydrazono]-1,3-dihydro-indol-2-one). The ligand was characterized by FTIR, UV-vis, mass, 1H-NMR, 13C-NMR, and CHN elemental analysis. New complexes of this ligand were created by treating methanol and a drop of DMF solution of the produced ligand with the hydrated metal salts of Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) in a molar ratio of 2:1 (L:M). As a result, complexes have been emerged and identified FTIR, UV-vis, C.H.N., chloride-containing, molar conductance, magnetic susceptibility, and atomic absorption. The characterization result for each complex indicated complexes wi
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