Journal of the Iranian Chemical Society
Volume:2 Issue: 3, Sept 2005

G-protein-coupled receptors (GPCRs) represent the largest known family of signal-transducing proteins and transmit signals for light and many extracellular regulatory molecules. GPCRs are dysfunctional or dysregulated in several human diseases and are estimated to be the targets of ~40% of the drugs used in clinical medicine today. Receptors for adenosine belong to this family, and so far four subtypes, the A1, A2A, A2B, and A3, have been recognized. The activation of adenosine receptors (ARs) is largely responsible for the variety of effects produced by adenosine throughout several organ systems. Based on the wide (and often beneficial) effects attributed to the accumulation of endogenously released adenosine,it has long been considered that regulation of ARs has considerable therapeutic potential. In this review, we focus on recent work on adenosine receptors as therapeutic targets and, in particular, on molecular modelling support to adenosine receptors targeting.

The anionic surfactant sodium n-dodecyl sulfate (SDS) plays a variety of roles with regard to protein conformation,depending on its concentration. SDS at low concentrations mostly induces the compaction of protein (folding). Examples of this include: the molten globule state of acid-unfolded cytochrome c, associated with enhancement of the exothermic enthalpy values of isothermal titration calorimetry and a reversible profile by differential scanning calorimetry; the enzyme activation and compaction of Aspergillus niger catalase, and relationship of calorimetric enthalpy (ΔHcal) to van''t Hoff enthalpy (ΔHVH), which proves the existence of intermolecular and intramolecular interaction during enzyme activation by SDS; the production of a new energetic domain for human apotransferrin and folded state for histone H1 by SDS. SDS at moderate concentrations below the critical micelle concentration (cmc) is a potent denaturant for protein in solution. Protein denaturation is a key method in thermodynamics and binding site analysis and can be used to enhance our understanding of the protein structure-function relationship. The interaction between protein and surfactant, such as SDS, at the cmc level is a complicated interaction, thermodynamically, that should bring about enthalpy correction through micellar dissociation and micelle dilution.

A simple and accurate spectrophotometric method for the determination of metronidazole in pure and pharmaceutical dosage forms has been developed. The proposed method is based on the reduction of the nitro group to amino group of the drug. This can be achieved by heating a mixture of an alcoholic solution of metronidazole, zinc powder and dilute hydrochloric acid in a water bath at 90 ± 5 °C for 15 min. The cold and clear filtrate reacts with p-benzoquinone to develop a purple color, which absorbs maximally at 526 nm. The calibration graph is linear over the concentration range of 15-190 µg ml-1 with a molar absorptivity of 1.09 × 103 l mol-1 cm-1. The proposed method is applied to commercially available pharmaceutical dosage forms and the results are statistically compared with those obtained by the reference method.

The present work describes the synthesis and characterization of some six and nine coordinated complexes of trivalent lanthanide(III) with 4[N-(2´-hydroxy-1´- naphthalidene)amino]antipyrinethiosemicarbazone (HNAAPTS). All the complexes have the general composition LnX3.n(HNAAPTS) (X = NO3-, n = 1; X = NCS- or ClO4-, n = 2). The complexes were characterized through elemental analyses, molar mass, conductivity measurements, magnetic susceptibilities, and infrared and electronic spectra. Infrared spectra revealed that HNAAPTS acts as a neutral tridentate (N,N,S) donor. The coordination number in these complexes is either six or nine depending on the nature of the anionic ligand.

Poly(acrylic acid) (PAA) samples with molecular weights between 820 and 2950 were synthesized by a solution polymerization process using an initiating redox system. The obtained PAAs were then screened for their ability to inhibit salt scale formation. In this screening system, salt scale was formed by injecting pit water into the oil. The salt scale inhibition efficiency was higher for PAAs at a higher concentration and for lower molecular weight PAAs. A reduction of pH, extension of stirring time, or an increase in temperature caused the inhibition efficiency of the PAAs to drop. An optimal inhibition efficiency of 98.70% was observed using a PAA with a molecular weight of 820 at a concentration of 20 ppm, at 20 °C, while being stirred for 1 h at a pH of 6.029.

Some new bromoquinazolinone substituted fluoran compounds were synthesized by the reaction of the keto acid, 2-(4-diethylamino-2-hydroxybenzoyl)benzoic acid with different 3-(3/4-hydroxyphenyl)-2-methyl/phenylbromo-4(3H) quinazolinones in the presence of a dehydration condensing agent like sulfuric acid. Various quinazolinones were prepared by reacting different monobromo/dibromobenzoxazine-4-ones with 3-aminophenol or 4-aminophenol in the presence of pyridine as a solvent. All the synthesized fluoran compounds were identified by conventional methods such as melting point, IR, 1H NMR, 13C NMR, elemental analysis and UV-visible spectroscopy in organic solvents and 95% acetic acid. All these colorless fluorans develop a color in contact with electron accepting compounds.

The kinetics of the oxidation of β-alanine by dihydroxydiperiodatoargentate(III) (DPA) in an alkaline medium was studied by spectrophotometry in a temperature range of 298.2 K-318.2 K. The reaction rate showed pseudo-first order dependence in the oxidant and 1 < nap < 2 in the reductant. A plausible mechanism involving a pre-equilibrium of adduct formation between the complex and reductant is proposed. The rate equations derived from the mechanism explain all experimental observations. The activation parameters along with the rate constants of the rate-determining step were calculated.

The present research discusses the structure stabilizing and protecting effects of Ni2+ against suicide-peroxide inactivation of horseradish peroxidase (HRP). Suicide inactivation of HRP by hydrogen peroxide (3 mM) was monitored by measuring change in the absorbance of the colored product (tetraguaiacol) of the catalytic reaction cycle at 470 nm. Progress curves of the catalytic reaction cycle were obtained at 27 °C, phosphate buffer (5 mM), pH 7.0. The corresponding kinetic parameters (e.g., initial enzyme activity (αo) and the apparent rate constant (ki) of suicide inactivation of HRP by peroxide) were evaluated using a kinetic equation derived in this study. Comparative activatory and inhibitory effects of Ni2+ on the kinetics of suicide-peroxide inactivation of HRP are discussed.

A modified electrode, which can be used as an anode for electrocatalytic oxidation processes of dyestuff in aqueous solutions, was fabricated by the electrodeposition of a lead oxide layer on a titanium substrate. The modified electrode was used for the electrochemical degradation of an acid green dye. The results of the electrocatalytic oxidation process of the dyestuff solutions were expressed in terms of the remaining dye concentration and chemical oxygen demand (COD) values. The different operating conditions of the treatment process were studied. The optimum operating conditions for the dye and modified electrode were determined, where good results for complete removal of the dye and COD were achieved. The optimum conditions were applied to the treatment of a sulfur black dye in true wastewater solutions.