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
Addition chloro acetyl isothiocyanate (C3H2ClNOS) with 3-Aminoaceto phenone (C8H9NO) to prepare a fresh Ligand [N-(3-acetyl phenyl carbamothioyl)-2-chloroacetamide](L). The ligand (L) behaves as bidentate coordinating through O and S donor with metal ions, the general formula of all complexes [M(L)2(Cl)2](M+2 = Manganese(II), Cobalt(II), Cadmium(II) and Mercury(II)). Compounds were investigation by Proton-1, Carbon -13 NMR spectra (ligand (L) only), Element Microanalysis for C, N, H, O, S, Fourier-transform infrared, UV visible, Conductance
This investigation is a study of the length of time where drops can exist at an oil-water interface before coalescence take place with a bulk of the same phase as the drops. Many factors affecting the time of coalescence were studied in is investigation which included: dispersed phase flow rate, continuous phase height, hole size in distributor, density difference between phases, and viscosity ratio of oil/water systems, employing three liquid/liquid systems; kerosene/water, gasoil/water, and hexane/water. Higher value of coalescence time was 8.26 s at 0.7ml/ s flow rate, 30cm height and 7mm diameter of hole for gas oil/water system, and lower value was 0.5s at 0.3ml/s flow rate, 10 cm height and 3mm diameter of hole for hexane
... Show MoreHand gestures are currently considered one of the most accurate ways to communicate in many applications, such as sign language, controlling robots, the virtual world, smart homes, and the field of video games. Several techniques are used to detect and classify hand gestures, for instance using gloves that contain several sensors or depending on computer vision. In this work, computer vision is utilized instead of using gloves to control the robot's movement. That is because gloves need complicated electrical connections that limit user mobility, sensors may be costly to replace, and gloves can spread skin illnesses between users. Based on computer vision, the MediaPipe (MP) method is used. This method is a modern method that is discover
... Show MoreIn this study, derivatives of polyvinyl alcohol (PVA) grafted with phthalic anhydride (PhA) and dyes were prepared to produce polymeric materials of PVA-g-PhA, PVA-g-PhA-anthocyanin, PVA-g-PhA-bromophenol blue, and PVA-g-PhAthymol blue. The materials were characterised by FTIR and 1 H NMR spectroscopies. The crystallinity of the polymers was evaluated with powder X-ray difraction, and the thermal stability by thermogravimetric analysis (TGA). The synthetic procedure for the polymeric materials entailed the formation of esters. The FTIR spectra of the polymers confrmed their formation since the ester carbonyl group stretch was observed at approximately 1691–1716 cm−1 in each material. NMR spectroscopy confrmed the addition of t
... Show MoreGiven the paucity and toxicity of available drugs for leishmaniasis, coupled with the advent of drug resistance, the discovery of new therapies for this neglected tropical disease is recognised as being of the utmost urgency. As such antimicrobial peptides (AMPs) have been proposed as promising compounds against the causative Leishmania species, insect vector-borne protozoan parasites. Here the AMP temporins A, B and 1Sa have been synthesised and screened for activity against Leishmania mexicana insect stage promastigotes and mammalian stage amastigotes, a significant cause of human cutaneous disease. In contrast to previous studies with other species the activity of these AMPs against L. mexicana amastigotes was low. This suggests that ama
... Show MoreOn the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.
Keywords: Coumarin-bas
... Show MoreThe objective of this research was to investigate the effect of replacing fat(shortening) with different percentages of tahena on the quality properties (physiochemical and sensory ) of shortened cake.The percentages of moisture,protein ,fat and ash of cake increased significantly(p<0.05) as the replacement was increased .The highest increase percentages were 10,48,5,and 90 %,respectivly, at 100% replacement .Carbohydrate,however,decreased by 10%at 100% replacement .these findings may indicate improvement of cake nutritional value.Standing height,as an indicator of cake volume, also increased significantly by 4% at the 50% replacement then it decreased by 4% 100% replacement level. Basic formula (control) has signific
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