Abstract
A modular replacement approach to the synthesis of sulfo-nucleotide analogs prepared from condensation of nucleoside aldehydes with bis phosphonate Horner-Wadsworth-Emmons reagents is disclosed. These analogs were shown to be inhibitors of Neisseria meningitidis CSS (NmCSS), which is a key enzyme in the biosynthesis of the capsular polysaccharides required for bacterial infection.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Cell Nucleus / metabolism
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Chemistry, Pharmaceutical / methods
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Cytoplasm / metabolism
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Humans
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Kinetics
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Models, Chemical
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N-Acylneuraminate Cytidylyltransferase / antagonists & inhibitors*
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N-Acylneuraminate Cytidylyltransferase / chemistry*
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Neisseria meningitidis / enzymology
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Nucleotides / chemistry
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Polysaccharides / chemistry
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Sulfones / chemistry*
Substances
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Enzyme Inhibitors
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Nucleotides
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Polysaccharides
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Sulfones
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N-Acylneuraminate Cytidylyltransferase