Etodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects compared to etodolac.
This research involved synthesis of new β-Lactam derivative from Azo compound[4-amino-N-(pyrimidine-2-yl)-3-(pyrimidine-2-yldiazenyl) benzene sulfonamide] (S1) record previously by many steps. Starting conversion the free amino group in an azo comp. to chloro acetamide derivative(S2), then reacted it with urea to give the oxazole ring derivative (S3) that which containing free amino group. The condensation reaction between the amino group and P-bromobenzaldehyde to produce Shiff base (B14). Finally staudinger's cyclo addition reaction go run between the Shiff base derivative (B14) and chloro acetyl chloride in the presence of tri ethyl amine (Et3N) as Base catalyst and dioxane a
... Show MoreThe Co (II), Ni (II) ,Cu(II), Zn(II) ,Cd(II) and Hg(II) complexes of mixed of amino acid (L-Alanine ) and Trimethoprim antibiotic were synthesized. The complexes were characterized using melting point, conductivity measurement and determination the percentage of the metal in the complexes by flame (AAS). Magnetic susceptibility, Spectroscopic Method [FT-IR and UV-Vis]. The general formula have been given for the prepared mixed ligand complexes [M(Ala)2(TMP)(H2O)] where L- alanine (abbreviated as (Ala ) = (C5H9NO2) deprotonated primary ligand, L- Alanine ion .= (C5H8NO2-) Trimethoprim (abbreviated as (TMP ) = C10H11N3O3S M(II) = Co (II),Ni(II) ,Cu(II), Zn(II) ,Cd(II) and Hg(II). The results showed that the deprotonated L- Alanine b
... Show MoreObjective: Schiff’s and Mannich bases of isatins are an important group of heterocyclic compounds which are of great importance in medicinal chemistry as antimicrobial agents. In the vision of these facts, new bis-Schiff bases and Mannich bases of isatins were synthesized. Methods: Three different bis-Schiff bases (3a-c) have been synthesized by reacting isatin, 5-fluoroisatin and 5-methoxy isatin with thiophene-2- carboxaldehyde using hydrazine hydrate to link between the carbonyl compounds, and then these bis- Schiff bases were condensed with two different secondary amines (piperidine and morpholine) separately, and formaldehyde to form the Mannich bases (4a-c and 5a-f), respectively. Results: The structures of the newly synthesized com
... Show MoreA new azo dye, 5,5-[1,2-phenylenebis(2,1-biazenediyl)]bis[8-quinolino], was synthesized by reacting the diazonium salt of o-phenylenediamine with 8-hydroxyquinoline. The ligand was subsequently used to prepare a series of metal complexes with V(IV), Fe(III), Cr(III), Mn(II), Mo(VI), and Ru(III). The ligand was characterized using 1H and 3C-NMR spectroscopy, while the metal complexes were analyzed using UV-Vis, FT-IR, and mass spectrometry, along with thermal analysis (TGA, DSC), (C.H.N.), conductivity measurements, magnetic susceptibility, and metal and chlorine content analysis, the results indicated that the ligand exhibits tetracoordination. The complexes predominantly formed octahedral geometries, except for the vanadium complex, which
... Show MorePeroxidase is a class of oxidation-reduction reaction enzyme that is useful for accelerating many oxidative reactions that protect cells from the harmful effects of free radicals. Peroxidase is found in many common sources like plants, animals and microbes and have extensive uses in numerous industries such as industrial, medical and food processing. In this study, P. aeruginosa was harvested to utilize and study its peroxidases. P. aeruginosa was isolated from a burn patient, and the isolate was verified as P. aeruginosa using staining techniques, biochemical assay, morphological, and a sensitivity test. The gram stain and biochemical test result show rod pink gram-ne
... Show MoreHeterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep
... Show MoreOral jelly is a semisolid preparation that could resolve problem associated withdosage form’s swallowing, especially in pediatric and elderly ones. This work aimedto prepare oral flurbiprofen (FBP) jelly to improve patient compliance. Heating andcongealing method was used to prepare FBP jelly using three different polymers (pectin,sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose). The effect ofdifferent concentrations of pectin and sucrose on jelly properties was studied. Theresults revealed that both pectin and sodium carboxymethyl cellulose polymers gaveacceptable jelly appearance and consistency. It was also observed that the increase ofpectin or sucrose concentration had a significant impact on jelly viscosity. All pe
... Show MoreBackground: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo
... Show MoreThe aim of present study was to develop gel formulation of microsponges of poorly soluble drug meloxicam (MLX) in order to enhance the release and dissolution of MLX which is the limitation for preparation in topical forms. Also skin delivery is an alternative administration for MLX that can minimize gastrointestinal (GI) side effects and improve patient compliance. The microsponges of MLX were prepared by quasi-emulsion solvent diffusion method. The effects of drug:polymer ratio, stirring time and Eudragit polymer type on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selec
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