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Volume 4, No. 4, December 2009, Thu Al-Hijja 1430 H

Articles

 

 

Efficient Synthesis of 2-Aroyl-3-Alkoxy-2,3-Dihydrothiazolo[2,3-c][1,2,4]Triazol-5(6H)-ones

Aryl carboxylic acid N'-(4-oxo-4,5-dihydro-thiazol-2-yl)hydrazides (4a-g) were prepared from the reactions of 2-carbethioxymethylthio-2-thiazoline-4-one (2) with alkyl or aryl hydrazides (3a-g), in ethanol at room temperature. The reactions of compounds 4a-g with methyl and ethyl orthoformates afforded 2-aroyl-3-alkoxy-2,3-dihydrothiazolo[2,3-c][1,2,4]triazol-5(6H)-ones (5a-n).

 

Mahmoud Al-Talib, Dalia Al-Saad,Mohanad Shkoor and Hasan I. Tashtoush*

 JJC, 2009, 4(4), 317-323

New Approach of Ethyl Substituted Isoquinoline-3-Carboxylate Synthesis

The synthesis of ethyl 1,4-disubstitued isoquinoline-3-carboxylate derivatives was achieved in four steps by employing Suzuki Miyaura reaction as a key step. The regiochemical outcome of the palladium catalysed cross-coupling reaction applied to a bis-triflate isoquinoline was reported. The present methodology can provide an expedient access to diversely substituted isoquinolines.

 

Michelyne Haroun*, Mohamad Abdul-Ghani, Christophe Tratrat

 JJC, 2009, 4(4), 325-327

Molecular Modeling Design, Synthesis and Biological Evaluation of New Imidazoline Derivatives Linked as α1-AR Antagonists and Ang II Receptor Antagonists

Two new series of 5-spiroalkyl-4-substituted-imidazoline derivatives connected to various 4-arylpiperazinyl-oxoethyl (XIa-g) and tetrazolyl (or cyano)biphenylyl-methylthio moieties (XIIa-e) were designed, synthesized, and biologically evaluated for their in vivo hypotensive activities. The design of compounds XIa-g was based upon the molecular modeling simulation fitting to the previously generated 3D α1-adrenoceptor (α1-AR) antagonists hypothesis using CATALYST (HipHop) modules. The simulation study revealed the high fitting affinities of these compounds to the α1-AR antagonists hypothesis and compound XIg showed the highest fitting affinity. The in vivo hypotensive activity of these compounds on normotensive cats was consistent with the results of molecular modeling study, where compound XIg exhibited the highest hypotensive activity at different doses. Meanwhile, the design of compounds XIIa-e was based upon the molecular modeling simulation fitting to the previously generated Ang II receptor antagonists hypothesis using catalyst (HipHop) modules. The simulation study revealed that the tetrazolyl analogues of the cyano precursors XIIa-e could be considered as promising hits, while the cyano precursors have low fitting affinities. As expected, the in vivo hypotensive evaluation of the cyano analogues indicated their low activity.

 

Mohamed A. H. Ismail*, Dalal A. R. Abou El Ella, Khaled A. M. Abouzid* and Deena S. M. Lasheen

JJC, 2009, 4(4), 329-347

          

A Thermodynamic Study of the Charge Transfer Complexes of C60
with some Crown Ethers

Formation of charge transfer complexes of [60]fullerene, C60, and crown ethers (1-4) in toluene was studied using Uv-Visible spectrophotometry. The stability constants and thermodynamic data of the resulting 1:1 complexes were determined. All charge transfer complexes formed were enthalpy stabilized, but entropy destabilized. The effect of donor atoms, their orientation, the substituents and the cavity size of the crown ethers on the formation constants and thermodynamic data are discussed.

 

Shehadeh A. Mizyed*, Deeb S. Marji and Enas Qarqaz

JJC, 2009, 4(4), 349-356

Development and Validation of Analytical Method for Fluconazole and Fluconazole Related Compounds (A, B, and C) in Capsule Formulations by HPLC with UV Detection

A simple and stability-indicating liquid chromatographic method was developed and validated for the analysis of Fluconazole and its related compound (A, B, and C) in capsule formulations. Liquid chromatography with a UV detector at a wavelength of 260 nm using a reversed-phase C18 column was employed in this study. Isocratic elution was employed using a mixture of methanol and water (40:60, v/v). This new method was validated in accordance with USP requirements for new methods for assay determination, which include accuracy, precision, specificity, linearity and range. The current method demonstrates good linearity over the range of 0.05-0.15 mg/ml of Fluconazole. The accuracy of the method is 99.3%. The precision of this method reflected by relative standard deviation of replicates is 0.61%. Validation of the same method for Fluconazole related compounds analysis was also performed according to USP requirements for quantitative determination of impurities which include accuracy, precision, linearity and range, selectivity, and Limit of quantitation (LOQ). Low LOQ of the related compounds using this method enables the detection and quantitation of these impurities at low concentration.

 

F. Al-Rimawi*

JJC, 2009, 4(4), 357-365

Indirect Voltammetric Method for Determination of Nitrogen Dioxide in the Ambient Atmosphere

A hydrodynamic voltammetrric method was developed to determine the concentration of atmospheric nitrogen dioxide. Air samples were collected in 0.1M NaOH scrubbing solution which converts NO2 to NO2- and NO3- in a fixed stoichiometric ratio. The produced NO2- ion was analyzed by hydrodynamic voltammetry at a rotating disk gold electrode. The Validity of the method was checked against spectrophotometric determination of NO2- . The agreement between the two methods was confirmed. The applicability of the method to real-life analysis was established by estimation of NO2 concentration in ambient air of three districts in Amman.

 

 

Muayad Esaifan and Mohammed Khair  Hourani*

JJC, 2009, 4(4), 367-375

Preparation and HPLC Analysis of the Natural Pigments Obtained from  Buckthorn (Rhamnus petiolaris Boiss) Dye Plants

In this work, the buckthorn natural pigments, namely aluminium, tin and iron-buckthorn were obtained by the reaction of KAl(SO4)2.12H2O, SnCl2.2H2O and FeSO4.7H2O solutions with buckthorn (Rhamnus petiolaris Boiss) berries. A reversed-phase high performance liquid chromatography (HPLC) with diode-array detection (DAD) method was utilized for the identification of the buckthorn natural pigments. The extraction of dyestuffs from the natural pigments was carried out with hydrochloric acid / methanol / water (2:1:1; v/v/v) solution. According to the results of HPLC analysis of the natural pigments, it was observed that both rhamnetin and emodin that present in the pigments were precipitated by Al(III) [1]  whereas only emodin was precipitated by Sn(II) and Fe(II). CIELAB values of the natural pigments were measured.

 

Ozan Deveoglu*, Recep Karadag and Turkan Yurdun*

JJC, 2009, 4(4), 377-385

Spectrophotometric Determination of Furosemide
in Pharmaceuticals Using Permanganate

Furosemide (FUR) was quantified upon treatment with a measured excess of permanganate in acid medium and unreacted oxidant being measured at 550 nm (3.0-24.0 g ml-1 FUR) or with known amount of permanganate in alkaline medium and the resulting manganate being measured at 610 nm (1.25-20.0 g ml-1 FUR).

 

Kalsang Tharpa, Kanakapura Basavaiah* and Kanakapura Basavaiah Vinay

JJC, 2009, 4(4), 387-397

1st Order Derivative Spectrophotometry Determination of Sertraline in Pharmaceutical Tablets by P-Chloranilic Acid

A new method has been developed for the determination of Sertraline in pharmaceutical tablets. A simple analytical procedure based on First Order derivative spectrophotometry of the colored product which was formed by charge transfer complexation of sertraline (n-donor) with π-acceptor chloranilic acid. First derivative spectrophotometry has been evaluated by measuring of the derivative signal at 475.72 nm 588.40 nm (peak to peak amplitude). Calibration graph was established for 5-100 g.mL-1 of sertraline with main percentage recoveries. The proposed method was applied successfully to the determination of sertraline in pharmaceutical tablet with good accuracy and precision.

 

 

Yousef  F. M. Alqahtani*, Abdullrahman A. Alwarthan,
Saad A. Altamrah

JJC, 2009, 4(4), 399-409