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.
Some metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato
... Show MoreExperimental study has been conducted for laminar natural convection heat transfer of air flow through a rectangular enclosure fitted with vertical partition. The partition was oriented parallel to the two vertical isothermal walls with different temperatures, while all the other surfaces of the enclosure were insulated. In this study a test rig has been designed and constructed to allow studying the effect of Rayleigh number, aperture height ratio, partition thickness, the position of aperture according to the side walls and according to the height, the position of the partition according to the hot wall, and partition inclination. The experiments were carried out with air as the working fluid for Rayleigh number range (5*107 – 1.3*10
... Show MoreIn this research, the dynamics process of charge transfer from the sensitized D35CPDT dye to tin(iv) oxide( ) or titanium dioxide ( ) semiconductors are carried out by using a quantum model for charge transfer. Different chemical solvents Pyridine, 2-Methoxyethanol. Ethanol, Acetonitrile, and Methanol have been used with both systems as polar media surrounded the systems. The rate for charge transfer from photo-excitation D35CPDTdye and injection into the conduction band of or semiconductors vary from a to for system and from a to for the system, depending on the charge transfer parameters strength coupling, free energy, potential of donor and acceptor in the system. The charge transfer rate in D35CPDT / the syst
... Show MoreTwo new ligands Na2[ H3B (BDIA)].0.05H2O (L1)(BDIA = 1-Boranyl-2,3-
Dihydro-1H-Indol-3-yl)]Acetic Acid and Na3[H2B(BDIA)2].0.3H2O.0.3CH3Ph (L2)
were synthesized by reaction of NaBH4 with indole -3- acetic acid (IAA) . The
coordination properties of ligands were studied with Co(II) , Ni(II) , Cu(II) and
Pt(IV) ions. Characterization and structural aspects of the prepared compounds were
elucidated by 1HNMR, FTIR electronic spectra, magnetic susceptibility, elemental
and metal analysis, thermal analysis (TG & DTG) and conductivity measurements.
The obtained data for metal complexes suggested square planar geometry for
copper complexes, octahedral geometry for nickel and platinium complexes and
tetrahedral geom
A new set of metal complexes by the general formula [M(C)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-chlorophenyl)succinamide] (C) derived from succinyl chloride with 4-Chloroaniline with the transition metal ions Mn(II), Co(II), Ni(II), Hg(II), Cu(II) and Cd(II). Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (C)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (C) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group) and the octahedral composition of these complexes is suggested. The anti-bacterial action of the compounds towards three types of bacteria
... Show MoreThree of imide intermediate products were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c) respectively in dry toluene with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the resulted products consider as
... Show MoreMeloxicam is a non-steroidal anti-inflammatory drug. It is practically insoluble in water. It is associated with gastrointestinal side effects at high doses on long term treatment. The aim of this investigation to formulate and evaluate gellified nanoemulsion of meloxicam as a topical dosage form to enhance meloxicam therapeutic activity and reduce systemic side effect.
The pseudo ternary phase diagrams were made, including the oil mixture which is composed of almond oil and peppermint oil at a ratio (1:2), variable surfactant mixture (S mix) which are tween 80 and ethanol at ratios of (1:1, 2:1, 3:1, and 4:1) and double distilled water. Slow dripping of double distilled water to the combination of the oil mixtu
... Show MoreIn this review, previous studies on the synthesis and characterization of the metal Complexes with paracetamol by elemental analysis, thermal analysis, (IR, NMR and UV-Vis (spectroscopy and conductivity. In reviewing these studies, the authors found that paracetamol can be coordinated through the pair of electrons on the hydroxyl O-atom, carbonyl O-atom, and N-atom of the amide group. If the paracetamol was a monodentate ligand, it will be coordinated by one of the following atoms O-hydroxyl, O-carbonyl or N-amide. But if the paracetamol was bidentate, it is coordinated by atoms (O-carbonyl and N-amide), (O-hydroxyl and N-amide) or (O-carbonyl and O-hydroxyl). The authors also found that free paracetamol and its complexes have antimicrobial
... Show MoreNew Schiff bases derived from D-galactose were synthesized by condensation of aldehyde (1,2:3,4-Di-O-isopropylidene-6-carboxaldehyde-α-D-galactopyranose) with different aromatic amines such as (4-bromo, 3-hydroxy, 4-iodo, 4-methoxy) aniline in dry benzene using glacial acetic acid as a catalyst. These compounds were converted to oxazepine derivatives by addition reaction with maleic anhydride in dry benzene as a solvent. The structures of the synthesized compounds have been characterized by elemental analysis, FTIR spectra, some of them by using 1HNMR spectra and measurement of its physical properties.