Rafidain Journal of Science

Tramadol is an opium analgesic drug that is used to relieve moderate to relatively severe pain. The major side effect of opium analgesic drugs is inhibit the intestinal peristalsis motility, and the effect of tramadol on gut motility is unknown quitely, therefore the effect of tramadol on intestinal peristalsis in vitro was examined in segments of the rabbit small intestine. Our study demonstrated that the low concentration of tramadol (0.1, 0.2, 0.3 , 0.4 , 0.5 ) ml , escort to activation peristalsis movement while increase the concentration (0.6, 0.7, 0.8, 0.9, 1.0 ) ml lead to decrease the contraction but when increase the concentration to 1ml lead to inhibited the peristalsis movement and complete relaxation. There for the study was concluded that the tramadol uses on rabbit small intestine decrease the peristalsis movement and this inhibition depend on concentration manner.

The aim of this study was to determine the antimicrobial effect of yarrow and it is flower extract on certain microorganisms. The ethanolic (alcoholic) extract of the flower and aqueous (water) extract was tested against: Pseudomonasa aeruginosa, Salmonella enterica enterica (Typhimurium), Shigella flexneri, Micrococcus luteus, Staphylococcus aureus and Enterococcus faecalis. Using the diffusion test, the alcoholic and aqueous flower extract at 200 mg /ml possessed abroad spectrum of antimicrobial activity against all tested microorganisms at different conc., alcoholic extract had the greatest inhibitory effect (diameter of inhibition zone) against Pseudo. aeruginosa 30 mm, Staph. aureus 24 mm and Micro. lutues 23 mm, While the aqueous extract slightly inhibited Pseudomonasa aeruginosa and Micrococcus luteus 12mm and 10 mm respectively compared with standard antibiotic Ciprofloxacin 26 mm, 22mm and 22mm but Entero. faecalis, S. enterica enterica (Typhimurium) and Shig. flexneri show high resistance for both extract 8 mm, 0 mm, 9 mm, 12 mm and 8 mm, 10 mm but sensitivity for Ciprofloxacin 23 mm, 30 mm and 31 mm. Minimum inhibitory concentration (MIC) were determined for alcoholic extract against sensitivite microorganisms: Pseudo. aeruginosa 50 mg/ml, Staph. aureus 100 mg/ ml and Micro. luteus 100mg/ ml. It could be concluded that the alcoholic extract of yarrow flower have considerable antimicrobial effect on some pathogenic which cause infection.

2-(α-Phenylacetyl) benzohydrazide (1) was prepared through the reaction of (Z)-3-benzylidene phthalide and hydrazine hydrate. Treatment of compound (1) with substituted benzoyl chloride yielded N'-aroyl-2-(α-phenyl acetyl) benzohydrazide (2a-e) which upon reaction with ammonium acetate provided the corresponding 2-phenyl-1-(2-(5-aryl-1,2,4-triazole-3-yl)phenyl)ethanones (3a-e). While the reaction of compound (1) with substituted benzaldehyde gave the hydrazones represented by N'-arylidene-2-(α-phenylacetyl) benzohydrazide derivatives (4a-f). Intramolecule cyclization of the latter compounds by means of acetic anhydride yielded 2-(α-phenylacetyl)phenyl-4-acetyl-4,5-dihydro-5-aryl-1,3,4-oxadiazoles (5a-f).
Compounds 2-(α-phenylacetyl)-N-(3,6-diphenyl-5-aryl-5,6-dihydro-1,2,4-triazine-4yl) benzamide (6a-f) were also obtained from the direct Diel-Alder reaction between dibenzylidine hydrazine as diene and compounds (4a-f) as dienophile enhanced by microwave irradiation.
The assigned structure of the prepared compounds were corroborated by available physical and spectral methods

A rapid, simple, and sensitive spectrophotometric and high performance liquid chromatographic methods have been developed for the quantitative determination of metoclopramide hydrochloride MCP in both pure and dosage forms. The spectrophotometric method is based on diazotization of MCP and then coupling with 2,4-dihydroxyacetophenone in alkaline medium. The resulting azodye exhibits maximum absorption at 450 nm with a molar absorptivity of 2.48 X 104 l.mol-1.cm-1. Beer's law is obeyed over the range 10-300µg/25 ml, i.e., 0.4-12 ppm with a relative standard deviation (RSD)of better than±1.092% and relative error better than -1.1%.
HPLC method has been developed for the measurement of MCP, the analysis was achieved on a C8 column using acetonitrile, water, and methanol in the ratio of 40:50:10 (V:V:V) (in the presence of 1% of sodium acetate) as a mobile phase by isocratic elution at 1 ml/min. flow rate, and detection was done spectrophotometrically at 308 nm. A linear relationship is obeyed over the range 0.18-0.8 ppm with a relative standard deviation (RSD) of better than 3.7% and relative error better than -1.6%.
Both methods were applied successfully to the assay of MCP in pharmaceutical preparations in the form of syrup, injection, and tablet.

2-Nitro-4-Methyl benzene sulphonyl chloride (I) has been prepared through sulphonation reaction from chlorosulphonic acid and o-nitrotoluene. Then compound (I) was allowed to react with primary and secondary amines to give a number of sulfonamide compounds (II1-14).
The synthesized compounds were identified depending on the physical and spectral data.

A series of new 2,5-disubstituted 1,3,4-oxadiazoles represented by compounds 2-phenyl-1-(2-(5-(5-aryl-1,3,4-oxadiazol-2-yl amino)-4H-1,2,4-triazol-3-yl)phenyl)ethanone (5a-f) have been synthesized from(Z)-3-benzylidene phthalide as useful precursor. 3-Benzylidene phthalide was reacted, firstly with urea under microwave irradiation and dry conditions to afford the corresponding 1-(2-(α-phenylacetyl)benzoyl)urea (1). The later compound underwent cycloaddition reaction with hydrazine hydrate (80%) to give 1-(2-(5-amino-4H-1,2,4-triazol-3-yl)phenyl)-2-phenylethanone (2), which upon reaction with ethyl chloroformate provided the corresponding ethyl- 5-(2-(α-phenylacetyl)phenyl)-4H-1,2,4-triazol-3-yl carbamate (3).
4-(5-(2-(α-Phenylacetyl)phenyl)-4H-1,2,4-triazol-3-yl) semicarbazide (4) was also prepared from the reaction of compound (3) with hydrazine hydrate (80%) under mild conditions. Finally, 2-phenyl-1-(2-(5-(5-aryl-1,3,4-oxadiazol-2-yl amino)-4H-1,2,4-triazole-3-yl)phenyl) ethanone (5a-f) were obtained via the reaction of compound (4) with various substituted benzoic acid by the action of phosphorous oxychloride. The structure of the prepared compounds were confirmed by the available physical and spectral methods

A simple, rapid and sensitive spectrophotometric method has been developed for the quantitative determination of metoclopramide hydrochloride in both pure form and in its pharmaceutical formulations. The method is based on diazotization of primary amine group of metoclopramide hydrochloride with sodium nitrite and nitric acid followed by coupling with 8-hydroxyquinoline in alkaline medium to form a pinkish – red coloured species, which showed a maximum absorption at 528 nm against reagent blank. Beer's law was obeyed over the concentration range of 5-300 μg / 25 ml. with a molar absorptivity 3.1×104 l.mol-1.cm-1. The method is suitable for the determination of metoclopramide hydrochloride in the presence of other ingredients that are usually present in dosage forms and the recoveries were obtained in the range of 98.9-100.0%. The method does not resort to temperature control or to solvent extraction. The effect of organic solvent on the spectrophotometric properties of the azo dye, the composition and stability constant have been worked out. The method has been successfully applied to the determination of metoclopramide in its pharmaceutical preparations ( tablet, syrup and drop ) .

To synthesis of some new heterocyclic compounds containing 1,3,4-thiadiazole moieties. Many of 5-alkyl-3-(4-substituted-2-butyn-1-yl) -1,3,4-thiadaizoline-2(3H)-one (15a-e and 16a-e) have been prepared by the reactions sequences starting from the acid hydrazides (1 and 2). All the products are well known for their useful biological activities. The structures of all compounds were confirmed by physical and spectral methods

The electrical behavior of association phenomena of tetra aqua (1,10 _ phenanthroline) zinc(II) chloride in methanol-water mixture have been investigated by precise conductance measurements at 288.15 - 308.15K which can give informations about ion-ion and ion-solvent interactions in solution. The limiting molar conductance λM2+ , the association constant KA and R the main distance between ions in solution as a results of those interactions can be calculated. Thermodynamics parameters (∆H, ∆G, ∆S) of the association processes and the coulombic forces which play an important role in the association process have been studied also.

Metal (II) complex of thiophene -2- carboxylic acid Hydrazide (TCH) ligand of the type [M(TCH)2X2] where M= Mn(II), Co(II), Ni(II),Cu(II), Zn(II) and Cd(II) , X=Cl-, NO3- have been prepared and characterized by metal analysis, molar conductance, magnetic moment measurements and electronic and IR spectral data. Based on physico- chemical studies, an octahedral geometry was assigned for all the complexes and the ligand (TCH) acted as neutral bidentate ligand, coordinating via the carbonyl oxygen and the amino nitrogen atoms.

The coupling reaction of sodium nitroprusside (SNP) with diazotized p-nitroaniline (DPNA) in basic media has been studied using spectrophotometric method. The intense yellow water-soluble associated species which was formed, showed maximum absorbance at 278 and 396 nm, depending on the concentration of SNP. Two calibration curves have been obtained for the determination of SNP with DPNA. The first curve (max=278 nm) obeys Beer's law over the range 25-300 µg/25 ml, with a regression equation of A=0.0027C+ 0.0747 ; R2 = 0.9853. The second curve (max=396 nm) obeys Beer's law over the range 300-5000 µg/25 ml, with a regression equation of A= 0.0002C+ 0.0439 ; R2=0.9943. The stability constants (K) were determined at different temperatures (283, 288, 293, 298 and 303K). Van't Hoof plot was obtained from which the thermodynamic parameters (free energy change ΔG, enthalpy change ΔH, and entropy change ΔS) were obtained.