The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydrolysis-kinetic study and pharmacological evaluation such as anti-inflammatory, ulcerogenecity as well as the effect of the NSAIDs in the central nervous system against degenerative mechanisms. The current study revealed that the umbelliferone conjugates of NSAIDs which upon administration would release the parent drug as a result of enzymatic or non-enzymatic hydrolysis in the desired site with enhanced anti inflammatory activity and reduction in the gastro intestinal toxicity. Also the synthesized pordrugs showed enhanced brain targeting efficiency with protective action against the degenerative processes.
Eriobotrya japonica Lindl., named as loquat, is a subtropical fruit tree of the family Rosaceae which is well known medical plant originated in Japan and China. Loquat portions, like leaves, peels and fruits have been shown to possess various health usefulnesses. In Chinese classical medicine, it is vastly utilized in many illnesses, like gastroenteric disorders, diabetes mellitus, pulmonary inflammatory diseases and chronic bronchitis. Loquat plant contain many active constituents, such as flavonoids, carotenoids, vitamins, polyphenolic compounds, other that have many biological effects like anti-tumor, anti-diabetic, anti-inflammatory, anti-mutagenic, antioxidant, antiviral, antitussive, hepatoprotective and hypoli
... Show MoreThe purpose of this research work is to synthesize conjugates of NSAIDs (ibuprofen, and naproxen) with sulfadiazine as possible mutual prodrugs to overcome the local gastric irritation of NSAIDs 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 bond that undergo reduction only by colonic bacterial azoreductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, 1H NMR, 13C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.
In this study we focused on the determination of influence the novel synthesized thiosemicarbazide derivative "2-(2-hydroxy-3-methoxybenzylidene) hydrazinecarbothioamide" (HMHC) influenced the corrosion inhibition of mild steel (MS) in a 1.0 M hydrochloric acid acidic solution.This is in an effort to preserve the metal material by maintaining it from corrosion.The synthesized inhibitor was characterized using elemental analysis, and NMR-spectroscopy. Then the corrosion inhibition capability of (HMHC) was studied on mild steel in an acidic medium by weight loss technique within variables [temperature, inhibitor concentration, and time]. The immersion periods were [1:00, 3:00, 5:00, 10:00, 24:00, and 72:00] hours and the tem
... Show MoreHistorically, medicinal herbs have been utilized as an important origin of chemicals with particular therapeutic potentials, and they continue to be a great place to find new medication candidates. Parthenocissus quinquefolia L. is a member of the grape-growing family Vitaceae. It is indigenous to Central and North America. It is widely dispersed in Iraqi gardens and plant houses from north to south. Traditionally, it has many uses, like relieving constipation, treating jaundice, expectorant, emetic, and others. At the same time, its proven activities include antioxidant activity, antimicrobial, anti-diabetic, thrombin inhibitor effect, and medicine for treating eyelid eczema. Parthenocissus quinquefolia contains valuable phytochemicals lik
... Show MoreA group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50
... Show MoreThis study concerned with phytochemical investigation and methods of extraction and separation of active constituents from Valeriana officinalis plant cultivated in Iraq. Due to the large number of active constituents in Valeriana officinalis, it was necessary to make analytical study of its constituents to determine the chemical nature of these constituents and then determine the main classes (terpenes and iridoids) using chemical reagents specific for each class. Different organic solvents like ethanol (70%) used in soxhlet apparatus and hexane, ethyl acetate and methanol were used separately to extract the main active constituents by maceration. Through comparison between these solvents using thin layer chromatograph
... Show More4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic
... Show MoreIn the current study, a direct method was used to create a new series of charge-transfer complexes of chemicals. In a good yield, new charge-transfer complexes were produced when different quinones reacted with acetonitrile as solvent in a 1:1 mole ratio with N-phenyl-3,4-selenadiazo benzophenone imine. By using analysis techniques like UV, IR, and 1H, 13C-NMR, every substance was recognized. The analysis's results matched the chemical structures proposed for the synthesized substances. Functional theory of density (DFT)
has been used to analyze the molecular structure of the produced Charge-Transfer Complexes, and the energy gap, HOMO surfaces, and LUMO surfaces have all been created throughout the geometry optimization process ut