Synthesis of 7-hydroxythioridazine and 7-hydroxysulforidazine

The thioridazine metabolites 7-hydroxythioridazine (2a) and 7-hydroxysulforidazine (2b) were synthesized. Commercial 4-chloro-3-nitrophenylmethylsulfone was converted to the corresponding 4-thiol through an intermediate xanthate ester. Subsequent zinc metal reduction provided the 3-amino thiolate. This salt was condensed with chloroquinone to yield 7-hydroxy-2-methylsulfonylphenothiazine which was then protected as the isopropyl ether. N-Alkylation with 2-(2-chloroethyl)-1-methylpiperidine using sodium hydroxide, then ether cleavage, afforded 2b . The N-alkylation followed by reduction with diisobutylaluminum hydride and deblocking yielded 2a . These reference standards will assist in an exploration of the potential role of meta-bolically formed 2a and 2b in the neuroleptic response to thioridazine.     

Growth of discontinuities in fluids with internal relaxation

The growth equation for weak discontinuities headed by wave fronts of arbitrary shape in a relaxing gas flow is derived along the orthogonal trajectories of the wave fronts. An explicit criteria for the growth and decay of weak discontinuities along their orthogonal trajectories is given. It is concluded that the internal relaxation processes in the flow as well as the wave front curvature both have a stabilizing effect on the tendency of the wave surface to grow into a shock in the sense that they cause the shock formation time to increase.     

Potential of Thermophilic Fungus Rhizomucor pusillus NRRL 28626 in Biotransformation of Antihelmintic Drug Albendazole

In the present investigation, thermophilic fungus Rhizomucor pusillus was used to study biotransformation of antihelmintic drug albendazole to produce its active metabolite, albendazole sulfoxide and novel metabolites of commercial interest. A two-stage fermentation procedure was followed for biotransformation of albendazole. The transformation was identified and structures were confirmed by high-performance liquid chromatography and liquid chromatography-tandem mass spectrometry analysis. Four metabolites albendazole sulfoxide, the active metabolite, albendazole sulfone, N-methyl metabolite of albendazole sulfoxide, and a novel metabolite were produced. The study demonstrates the biotransformation ability of thermophilic fungus R. pusillus NRRL28626 in the production of, the active metabolite of albendazole which has industrial and economic importance, other metabolites and a novel metabolite in an ecofriendly way.     

Nano-structured nickel oxide based DNA biosensor for detection of visceral leishmaniasis (Kala-azar)

Sol-gel synthesized nickel oxide (NiO) film deposited onto indium tin oxide (ITO) coated glass plate has been utilized for the development of sensitive and stable DNA biosensor and demonstrated for diagnosis of visceral leishmaniasis also known as Kala-azar. Leishmania specific sensor is developed by immobilizing 23mer DNA sequence (oligonucleotide) identified from 18S rRNA gene sequences from Leishmania donovani. Characterization studies like X-Ray Diffraction and Scanning Electron Microscopy revealed the formation of nano-structured NiO, while immobilization of single strand (ss)-DNA of Leishmania was supported by UV-visible, Fourier Transform Infrared Spectroscopy and Scanning Electron Microscopy techniques. Response studies of ss-DNA/NiO/ITO bioelectrode are carried out using differential pulsed voltammetry in presence of methylene blue redox dye as a redox mediator. A linear response is obtained in the wide concentration range of 2 pg ml(-1) to 2 μg ml(-1) of complementary target genomic DNA (disease DNA) within the variation of 10% for 5 sets of studies. The observed results hold promise not only for diagnosis of Kala-azar patients but also hold enormous potential of the nano-NiO based probe for development of stable and sensitive biosensors.     

Nonlinear breaking of waves in an electrically conducting and radiating gas

The effects of radiative transfer are treated by the use of a differential approximation which is valid over the entire optical depth range from the transparent limit to the optically thick limit. The singular surface theory is used to determine the modes of wave propagation and to evaluate the behaviour at the wave head. It is shown that there are two modes of wave propagation namely (i) the radiation induced waves which are always damped, and (ii) the modified magnetogasdynamic waves which break at the wave front if the initial discontinuity is sufficiently strong. The effects of thermal radiation, the magnetic field intensity, the finite electrical conductivity and the initial wave front curvature on the non-linear breaking of modified magnetogasdynamic waves are discussed.

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Zusammenfassung Der Einfluß der Strahlung wird mit Hilfe von Differential-Näherungen behandelt, die im ganzen Bereich von optischen Tiefen Gültigkeit haben, von der Transparenz bis zur optisch dicken Grenze. Die Theorie singulärer Flächen wird benützt um die Wellenausbreitung und das Verhalten an der Wellenfront zu behandeln. Es wird gezeigt, daß es zwei Formen von Wellenausbreitung gibt, nämlich (i) Wellen erzeugt durch Strahlung, die immer gedämpft sind, und (ii) die modifizierte magnetogasdynamische Welle, die an der Front immer bricht, wenn die ursprüngliche Diskontinuität stark genug ist. Es werden die Einflüsse der Wärmestrahlung, der magnetischen Feldstärke, der endlichen elektrischen Leitfähigkeit und der ursprünglichen Wellenkrümmung auf die nicht-lineare Frontbildung untersucht.

     

Nitro group participation in the formation of heterocycles

Benzoyl bromide (2-nitrophenyl) hydrazone (2) was treated with sodium ethoxide and ethyl cyanoacetate and two unexpected products were obtained. These products were ultimately shown to be 6-bromo-3-phenyl-1,2,4-benzotriazine (32) and 5-bromo-2-phenylbenzoxazole (38), by comparison with authentic samples which were synthesized. A mechanism is presented for the formation of these two heterocyclic systems (32 and 38) from 2.     

Chalcones XI: Potential Germicides Derived from Acetyl Phenanthrenes and Acetophenones

Thirteen phenanthryl and biphenylyl chalcones have been synthesized in presence of saturated solution of Na in methanol to evaluate their germicidal activity against gram +ve and ?ve bacteria.