This research, involved a series of some new compounds containing different hetero cyclic new pentagonal and hexagonal rings, through the reaction of 2-mercapto-3-phenyl-4(3H)quinazolinone (1) with chloroacetylchloride in the presence of potassium hydroxide, and dry dimethylformamide (DMF) as a solvent to obtain the intermediate compound (2). This compound is reacted with different reagents to give four routes, the first route include direct reaction with substituted-2-aminobenzothiazole under certain conditions to give new compounds (3-9). The second route involved condensation compound (2) with 5-substituted-2-amino-1,3,4-oxadiazole in the presence of potassium carbonate anhydrous to give new compounds (10-13).while the third route involved condensation compound (2) with para-phenylenediamine in ethanol as a solvent to give the corresponding compound (14) which the conversion new substitutes 1,2,3-triazole compounds (17-18) were prepared through the reaction of compound (14) with different reagent to give compounds (15-16). And subsequent reactions to obtain compounds (17-18) respectively. The fourth route include reaction compound (2) with para-chlorosulphonylaniline to give compound (19) which the conversion new sulphanilamide compounds (20-22) were prepared through the reaction compound (19) with different primary aromatic amine. The structure of newly synthesized compounds were identified by spectral methods their [FTIR,1HNMR, 13C-NMR] and measurements some of its physical properties and some specific reactions. Furthermore were studied the effects of the preparing compounds on some strains of bacteria and fungicidal.
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
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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
(1)
Leishmaniasis is a disease caused by a protozoan parasite of the genus Leishmania. It is transmitted by the bite of sandfly (Subfamily Phlebotominae). Limited drugs are available for the treatment of leishmaniasis, and the general drug (pentostam) have many side effect on patients. Therefore, there is an urgent need for another drugs for the treatment of leishmaniasis.
This study aimed to develop new type of antileishmanial agents instead of classical drug (pentostam) and investigated the effectiveness of silver nanoparticles (Ag NPs) on Leishmania tropica parasites in both phases promastigote and amastigote in comparision to pentostam in in vitro condition.
This study showed the effects of Ag NPs in comparision to pentostam with d
New metal ions complexes of tridentate ligand (1-((dicyclohexylamino) methyl)-3-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrzol-4-ylimino) indolin-2-one) have been synthesized and characterized by chemical-physical analysis. The ligand acts as a tridentate for the complexation reaction with all metal ions. The new complexes, possessing the general formula [M(L)Cl]Cl where M=[Ni(II), Cu(II), Zn(II), Pd(II), Cd(II), Pt(IV) and Hg(II) ] ,show tetrahedral geometry. All complexes ,except Pd(II) complex which has a square planar geometry and Pt(IV) which show an octahedral geometry. The geometry of the prepared compounds has been proposed in another method theoretically by using one of the calculation molecular programs (Hype
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The complexes Shiff base and mixed ligands complexes of bipyridyl and Schiff base 1,5-dimethyl-4-(5-oxohexan-2-ylideneamino)-2-phenyl-1H-pyrazol-3(2H)-one (L) with Cr(III), Mn(II), Fe(II) and Co(II) were prepared. The compounds have been characterized by FT-IR, UV-Vis, mass and 1H and 13C-NMR spectra, magnetic moment, elemental microanalyses (C.H.N.), chloride containing, atomic absorption and molar conductance. The studies made are indicating towards octahedral geometry for these complexes. Hyper Chem-8 program has been used to prediction structural geometries of compounds in gas state, the heat of formation, binding energy, total energy and electronic energy and dipole moment at 298oK. The c
... Show More2,2'-(1-(3,4-bis(carboxydichloromethoxy)-5-oxo-2,5-dihydrofuran-2-yl)ethane-1,2-diyl)bis(oxy)bis(2,2-dichloroacetic acid) a derivative of L-ascorbic acid was prepared by reaction of L-ascorbic acid with trichloroacetic acid (1:4) ratio, in the presence of potassium hydroxide. A series of new metal complexes of this ligand were prepared by a reaction with the chlorides of Cd(II), Co(II), Ni(II), Cu(II) and Zn(II). The new ligand and its complexes were identified by C.H.N., IR, UV-visible spectra, Thermogravimetric analysis (TGA), as well as 1H, 13C-NMR and Mass spectra for ligand L. The complexes were also identified by molar conductance, atomic absorption, magnetic susceptibility and X-ray diffraction for Cu (II) complex. FT-IR spectra
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