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)
In the present paper we report the synthesis of a new ligand [HL][(2-1-[(2-hydroxy-benzylidene)-hydrazono]-ethyl) benzene-1, 3, 5-triol and its complexes with (Mn", Fe", Cd", and Hg") The ligand was prepared in two steps. In the first step a solution of salicylaldehyed in methanol reacted under reflux with hydrazinemonohydrate to give an intermediate compound which reacted in the second step with 2, 4, 6-trihydroxidernonohydrate giving the tientioned ligand. The complexes were synthesis by direct reaction of the corresponding metal chloride with ligand. The ligand and the complexes have been characterized by spectroscopic methods [" H NMR, IR, UV-Vis,, atomic absorption], HPLC microanalysis along with conductivity measurements. From the abo
... Show MoreThis work comprises the synthesis of new thioxanthone derivatives containing C-substituted thioxanthone. To obtain these derivatives, the o-mercapto benzoic acid was chosen as the starting material, which was reacted with dry benzene in sulfuric acid (98 %) to produce the thioxanthone (1). The 2,7-(disulfonyl phosphine imine) thioxanthone (4-8) were prepared from reaction of compound (1) with chlorosulfonic acid gave 2,7-(disulfonyl chloride) thioxanthone (2). Treatment of (2) with sodium azide to produce 2,7-(disulfonyl azide) thioxanthone (3). Condensation of (3) with phosphorus compounds afforded compounds (4-8). The 2,7-(disulfonamide) thioxanthone (9-21) was obtained when co
... Show MoreIn contrast to the classical antibacterial sulfa drugs that are unsubstituted or monosubstituted, our newly synthesized analogs were designed to obtain sulfonamide moiety containing disubstituted hetero nitrogen atom. These compounds were formed successfully by chlorosulfonation of acetanilide and the product was treated with different cyclic amines and finally amide hydrolysis was necessary to get agents that were analyzed for IR, UV, CHN, melting points and solubility. At last, we studied their antibacterial activity on certain types of bacteria and we noticed the inactivity due to possible steric factor. Principly, this means these products have no inhibiting action against the used microbes.
The reaction of some new Schiff bases ( 2-[(2-Amino – ethylimino)-methyl]-R , 2-({2-[(R-benzylidene)-amino]-ethylimino}-methyl)-R with Benzoyl chloride or Acetyl chloride were carried out. Subsequent reactions of these products N-(2-Amino-ethyl)-N-[Chloro-(R) –methyl]-benzamide or N-(2-{?-[chloro-(R) –methyl]-amino}-ethyl)-N-[chloro-(R) –methyl]- benzamide with thiourea afforded thioureas compounds. The synthesized compounds were confirmed by their IR,UV,spectra and C.H.N. analysis.
G-system composed of three isolates G3 ( Bacillus),G12 ( Arthrobacter )and G27 ( Brevibacterium) was used to detect the mutagenicity of the anticancer drug, cyclophosphamide (CP) under conditions similar to that used for standard mutagen, Nitrosoguanidine (NTG). The CP effected the survival fraction of isolates after treatment for 15 mins using gradual increasing concentrations, but at less extent comparing to NTG. The mutagenic effect of CP was at higher level than that of NTG when using streptomycin as a genetic marker, but the situation was reversed when using rifampicin resistant as a report marker. The latter effect appeared upon recording the mutagen efficiency (ie., number of induced mutants/microgram of mutagen). Measuring the R
... Show MoreThis research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4- tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2)
... Show MoreIn recent years, the consideration of natural products as anti-inflammatory and antioxidative treatments has more interested worldwide. Moreover, natural products are easily obtained and are relatively safe the Royal jelly (RJ) is one of them. The current study was carried to evaluate the effects of pregabalin (PGB) on physiological activity of sperms, reproductive hormones assay and some biochemical analysis. Forty (40) male albino rats (10-weeks-old) were divided into four groups (10 rats each): G1 (treated with PGB drug, 150 mg/kg B.wt (Lyrica-Pfizer-Pharmaceutical Industries), G2 (treated with RJ 1g/kg), G3 (treated with PGB drug and RJ together), and G4 control treated with norma
2-(2-amino-5-nitro-phenylazo) -phenol was ready by grouping the diazonium salt of 2-aminophenol with 4-nitroaniline.Thegeometry of azo ligand(HL)was resolved on the origin of (C.H.N) analysis, 1H and 13CNMR spectra, infrared spectra and UV–vis electronic absorption spectra. Dealing with the azo ligand produced with Nd+3,Cd+3,Dy+3 and Er+3at aqueous ethanol for a 1:2 metal: ligand rate, and in perfect ph. The formation for compounds have been described by utilizing flame atomic absorption,(C.H.N) Analyses, conductivity, infrared spectra and UV–vis spectral procedures. Nature in the produced compounds have been studied obey the ratio of mole and continuous variance manners, Beer's law yielded up a concentration rate (1×10-4 - 3×10-4M) .
... Show More6-(2-benzathiazolyl azo),-3,5-dimethylphenol was formed by grouping the 2- benzothiazole diazonium chloride with 3,5-dimethylphenol. Azo ligand(L) was resolved on the origin by 1H and 13CNMR, FTIR and UV-V is spectral analysis. Complexation of tridentate ligand (L) with Co2+, Ni2+, Cu2+ and Zn2+ in aqueous of ethyl alcohol with a 1:2 metal:ligand, and at ideal pH.. The formation of metal chelates are assigned using flame atomic, absorption, FTIR, and UV-Vis spectral analysis, other than conductivity and magnetic estates. The nature of the metal chelates were carried out by mole ratio and continuous, variation mechanism, Beer's law, followed the rate (0.0001 - 3×0.0001 M) concentration., High molar, absorptivity, for the complex solutions w
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