25 research outputs found
Tautomerism and geometric isomerism of nitrogen containing derivatives of carbonyl compounds
No full textStudy of Differences in the Reactivity of Alkyl and Aryl Nitrones Derived from 4-oxo-4 H
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A Facile Cleavage of the Carbon-Nitrogen Bond of Aromatic Imines Using Acylation Reagents in the Presence of Catalytic Amounts of Ytterbium Triflate
No full textStudies of the tautomerism and geometrical isomerism of nitrogen-containing derivatives of carbonyl compounds I. Polarographic study of the transformations of some phenylhydrazones in methanol
No full textARYL AZIDES AS PROTEIN PHOTOLABELS: ABSORPTION SPECTRAL PROPERTIES AND QUANTUM YIELDS OF PHOTODISSOCIATION
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A new synthesis of alkene-containing minor-groove binders and essential hydrogen bonding in binding to DNA and in antibacterial activity
No full textA practical synthesis of alkene-containing minor-groove binders for DNA, related to distamycin, with potential for wide structural diversity is described, based upon the Wittig chemistry of N-alkylpyrrole aldehydes. The compounds prepared have been evaluated for binding to DNA by physical methods (melting temperature and NMR) and for their antibacterial activity. Significantly, it was found that alkenes linking the aryl head group of the minor-groove binder promote strong binding to DNA and high antibacterial activity against Gram-positive bacteria. Conversely, a minor-groove binder containing an alkene located towards the alkylamino tail group has a low affinity for DNA and does not show antibacterial activity. These observations suggest an important role for specific hydrogen bonds in the binding of compounds of this type to DNA, and in their antibacterial activity
