Effect of Sodium Dodecylbenzenesulfonate on the Association Behavior of Promethazine Hydrochloride in Aqueous/Electrolyte Solutions at Different Temperatures

The interaction between the amphiphilic phenothiazine drug promethazine hydrochloride (PMT) and an anionic surfactant sodium dodecylbenzenesulfonate has been investigated using the conductometric technique in the absence and presence of an inorganic salt (50 mmol·kg^?1 NaCl) at five different compositions and temperatures. PMT is employed for the cure of allergic symptoms. Different physicochemical parameters such as critical micellar concentration (cmc), thermodynamic, and micellar composition are evaluated and discussed in detail using regular solution theory (RST). The addition of salt decreased the surface charge of micelles, lowering the cmc values of the amphiphile. The interaction parameter (β) is negative at all temperatures and compositions indicating attractive interactions. Due to the presence of NaCl in mixed systems the attractive interaction (β) was further increased (β values more negative). The negative values of Gibbs energy (\( \Delta G^{0}_{\text{m}} \)) of mixing revealed the stability of the solution. Owing to the presence of NaCl, the \( \Delta G^{0}_{\text{m}} \) values are found to be more negative suggesting that the driving force for interaction was significantly increased and micellization more thermodynamically favorable.     

Synthesis and spectroscopic characterization of novel 2-amino-4,5,6,7-tetrahydro-3H-cyclopenta[d]pyrimidine and pyrimido[1,2-a]pyrimidine derivatives

2-Aminocyclopenta[d]pyrimidines 3a-c were achieved via a one-pot, three-component reactions of cyclopentanone 1, aromatic aldehyde and guanidine hydrochloride (1:2:1 molar ratio). Also, cyclization of 2,5-bis-(arylmethylidene)cyclopentanones 2 with guanidine hydrochloride (1:1 molar ratio) in methanol in the presence of sodiummethoxide afforded cyclopenta-[d]pyrimidines 3. Compound 3a has been shown to be a useful building block for the synthesis of some novel pyrimido[1,2-a]pyrimidines 5, 7 and 12. The structures of the newly synthesized compounds were confirmed on the basis of analytical and spectral data.     

Electric impedance study of elastic alternating propylene-carbon monoxide copolymer (PCO-200)

The electrical properties of elastic alternating propylene-carbon monoxide copolymer (PCO-200) were investigated using the impedance spectroscopy technique. The results revealed a phase transition at about 70 °C where the material transforms from its insulating phase of conductivity in the order of 6×10⁻⁹ to about 9×10⁻⁵ (Ω m)⁻¹, The second phase is characterized by temperature dependent electrical relaxation phenomena. The plot of the complex electric modulus and the complex impedance yields semicircles in the temperature range 70 up to 110 °C and a decreasing radius with increasing temperature. The activation energy was found to be in the order of 0.8 eV.     

Synthesis of DNA interstrand cross-links using a photocaged nucleobase

The missing linking: BCNU is a chemotherapy drug that generates an ethylene bridge between N(1) of deoxyguanosine and N(3) of deoxycytidine. No synthesis of a DNA containing this moiety has been reported until now. A new strategy uses a photocaged nucleobase that, when released, generates a highly reactive intermediate which cross-links the opposing DNA strand in a manner analogous to BCNU (see scheme, NBOC=ortho-nitrobenzyloxycarbonyl).     

Hole mediated coupling in Sr2Nb2O7 for visible light photocatalysis

The band gap reduction and effective utilization of visible solar light are possible by introducing the anionic hole-hole mediated coupling in Sr(2)Nb(2)O(7). By using the first principles calculations, we have investigated the mono- and co-anionic doping (S, N and C) in layered perovskite Sr(2)Nb(2)O(7) for the visible-light photocatalysis. Our electronic structure and optical absorption study shows that the mono- (N and S) and co-anionic doped (N-N and C-S) Sr(2)Nb(2)O(7) systems are promising materials for the visible light photocatalysis. The calculated binding energies show that if the hole-hole mediated coupling could be introduced, the co-doped systems would be more stable than their respective mono-doped systems. Optical absorption curves indicate that doping S, (N-N) and (C-S) in Sr(2)Nb(2)O(7) can harvest a longer wavelength of the visible light spectrum as compared to the pure Sr(2)Nb(2)O(7) for efficient photocatalysis.     

EPR Spectroscopy of 4, 4′‐Bis(tert‐butyl)‐2, 2′‐bipyridine‐1, 2‐dithiolatocuprates(II) in Host Lattices with Different Coordination Geometries

A series of new heteroleptic MN₂S₂ transition metal complexes with M = Cu²⁺ for EPR measurements and as diamagnetic hosts Ni²⁺, Zn²⁺, and Pd²⁺ were synthesized and characterized. The ligands are N₂ = 4, 4′‐bis(tert‐butyl)‐2, 2′‐bipyridine (tBu₂bpy) and S₂ =1, 2‐dithiooxalate, (dto), 1, 2‐dithiosquarate, (dtsq), maleonitrile‐1, 2‐dithiolate, or 1, 2‐dicyanoethene‐1, 2‐dithiolate, (mnt). The Cu^II complexes were studied by EPR in solution and as powders, diamagnetically diluted in the isostructural planar [Ni^II(tBu₂bpy)(S₂)] or[Pd^II(tBu₂bpy)(S₂)] as well as in tetrahedrally coordinated[Zn^II(tBu₂bpy)(S₂)] host structures to put steric stress on the coordination geometry of the central CuN₂S₂ unit. The spin density contributions for different geometries calculated from experimental parameters are compared with the electronic situation in the frontier orbital, namely in the semi‐occupied molecular orbital (SOMO) of the copper complex, derived from quantum chemical calculations on different levels (EHT and DFT). One of the hosts, [Ni^II(tBu₂bpy)(mnt)], is characterized by X‐ray structure analysis to prove the coordination geometry. The complex crystallizes in a square‐planar coordination mode in the monoclinic space group P2₁/a with Z = 4 and the unit cell parameters a = 10.4508(10) Å, b = 18.266(2) Å, c = 12.6566(12) Å, β = 112.095(7)°. Oxidation and reductions potentials of one of the host complexes, [Ni(tBu₂bpy)(mnt)], were obtained by cyclovoltammetric measurements.     

Studies of the Rate Constant of l-DOPA Oxidation and Decarboxylation by HPLC

The objective of current investigation was to study the degradation behavior of l-DOPA under different conditions by high performance liquid chromatography (HPLC), and to develop and validate a stability-indicating HPLC method. The developed RP-HPLC method was validated with respect to linearity, accuracy, precision and specificity. Oxidation was found to occur in alkaline and to some extent in thermal conditions, while the drug was stable when incubated at acidic conditions and under photolytic stress. The oxidation of l-DOPA was observed to follow first-order kinetics. The degradation rate constants and half-life were calculated. The cytotoxicity and enzymatic degradation of l-DOPA was examined using the human intestinal epithelial Caco-2 cells. The drug was rapidly decarboxylated by aromatic amino acid decarboxylase to dopamine. The conversion of l-DOPA to dopamine was dose- and time-dependent.

     

Spectrophotometric and Fluorimetric Methods for the Determination of Methoxamine Hc1 in Bulk Drugs and in Ampoules

Abstract

Three simple and sensitive methods for the determination of methoxamine HCl in bulk drugs and in ampoules were proposed. The methods are based on the oxidation of methoxamine HCl by sodium periodate, potassium permanganate and cerium(IV)sulphate. The first two reactions are followed spectrophotometrically by measuring the absorbance at 352 &; 608 nm for the periodate and permanganate methods, respectively. The third method is based on measuring the relative fluorescence intensity of Ce(III)arising from Ce(IV) at 348 nm with excitation wavelength at 257 nm. The different experimental parameters were carefully studied. Under the described conditions the proposed methods were applicable over the concentration ranges 10.0 - 40.0, 2.0-10.0 and 0.05-0.30 μg ml^?1 for the three methods, respectively.     

Synthesis and Cytotoxic Activity Study of Novel 2-(Aryldiazenyl)-3-methyl-1H-benzo[g]indole Derivatives

A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a–f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a–f) were characterized using ¹H NMR, ¹³C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 µM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.