924 resultados para chiral drugs


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We consider the minimal chiral Schwinger model, by embedding the gauge non-invariant formulation into a gauge theory following the Batalin-Fradkin-Fradkina-Tyutin point of view. Within the BFFT procedure, the second-class constraints are converted into strongly involutive first-class ones, leading to an extended gauge-invariant formulation. We also show that, like the standard chiral model, in the minimal chiral model the Wess-Zumino action can be obtained by performing a q-number gauge transformation into the effective gauge non-invariant action.

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The present study evaluated in vitro susceptibility testing of dermatophytes isolates from healthy cattle and soil samples against three antifungal agents and three topical veterinarian drugs. Itraconazole and terbinafine showed a higher in vitro fungicidal activity than fluconazole. The veterinarian drugs LEPECID (R) and iodine 5% were more active in vitro than the UNGUENTO (R) spray. All drugs showed fungicidal activity against Microsporum gypseum, and they may be considered as efficient agents for the topical treatment of dermatophytoses in cattle.

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The coumarin antibiotics are potent inhibitors of DNA replication whose target is the enzyme DNA gyrase, an ATP-dependent bacterial type II topoisomerase. The coumarin drugs inhibit gyrase action by competitive binding to the ATP-binding site of DNA gyrase B protein. The production of new biologically active products has stimulated additional studies on coumarin-gyrase interactions. In this regard, a 4.2 kDa peptide mimic of DNA gyrase B protein from Escherichia coli has been designed and synthesized. The peptide sequence includes the natural fragment 131-146 (coumarin resistance-determining region) and a segment containing the gyrase-DNA interaction region (positions 753-770). The peptide mimic binds to novobiocin (K-a = 1.4 +/- 0.3 x 10(5) m(-1)), plasmid (K-a = 1.6 +/- 0.5 x 10(6) m(-1)) and ATP (K-a = 1.9 f 0.4 x 10(3) m(-1)), results previously found with the intact B protein. on the other hand, the binding to novobiocin was reduced when a mutation of Arg-136 to Leu-136 was introduced, a change previously found in the DNA gyrase B protein from several coumarin-resistant clinical isolates of Escherichia coLi. In contrast, the binding to plasmid and to ATP was not altered. These results suggest that synthetic peptides designed in a similar way to that described here could be used as mimics of DNA gyrase in studies which seek a better understanding of the ATP, as well as coumarin, binding to the gyrase and also the mechanism of action of this class of antibacterial drugs. Copyright (C) 2004 European Peptide Society and John Wiley Sons, Ltd.

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Alzheimer's disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays, drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by regulation of the synthesis and release of acetylcholine in the brain. There are only four commercial medicines approved for treatment of AD, and natural products have played an important alternative role in the research for new acetylcholinesterase inhibitors, as exemplified through the discovery of galantamine. This profile conducts us to give in this paper an overview relating the several classes of natural products with anti-cholinesterasic activity as potential templates to the design of new selective and powerful anti-Alzheimer drugs.

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We study a new mechanism for the electromagnetic gauging of chiral bosons showing that new possibilities emerge for the interacting theory of chiral scalars. We introduce a chirally coupled gauge field necessary to mod out the degree of freedom that obstructs gauge invariance in a system of two opposite chiral bosons soldering them together.

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Using a form of the effective potential for composite operators with a variational approach we show that it is possible to get different directions of the chiral phase transition in QCD. Which one occurs depends on the way the Schwinger-Dyson equation for the fermion self-energy is used in the 2-loop term of the effective potential. We must choose the 2-loop term which agrees with phenomenology in each form of the effective potential.

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We argue that the minimal chiral background for the two-pion exchange nucleon-nucleon (NN) interaction has nowadays a rather firm conceptual basis, which entitles it to become a standard ingredient of any modern potential. In order to facilitate applications, we present a parametrized version of a configuration space potential derived previously. We than use it to assess the phenomenological contents of some existing NN potentials.