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5. MRSA Isolates from United States Hospitals Carry dfrG and dfrK Resistance Genes and Succumb to Propargyl-Linked Antifolates

Author

Reeve, Stephanie M., primary, Scocchera, Eric W., additional, G-Dayanadan, Narendran, additional, Keshipeddy, Santosh, additional, Krucinska, Jolanta, additional, Hajian, Behnoush, additional, Ferreira, Jacob, additional, Nailor, Michael, additional, Aeschlimann, Jeffrey, additional, Wright, Dennis L., additional, and Anderson, Amy C., additional

Published
2016
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7. Direct Substitution of Arylalkynyl Carbinols Provides Access to Diverse Terminal Acetylene Building Blocks.

Author

G-Dayanandan, Narendran, Scocchera, Eric W., Keshipeddy, Santosh, Jones, Heather F., Anderson, Amy C., and Wright, Dennis L.

Subjects
*TRIMETHOPRIM, *SUBSTITUTION reactions, *METHANOL, *ACETYLENE, *METHYLATION, *NUCLEOPHILIC addition (Chemistry)
Abstract

To develop next generation antifolates for the treatment of trimethoprim-resistant bacteria, synthetic methods were needed to prepare a diverse array of 3-aryl-propynes with various substitutions at the propargyl position. A direct route was sought whereby nucleophilic addition of acetylene to aryl carboxaldehydes would be followed by reduction or substitution of the resulting propargyl alcohol. The direct reduction, methylation, and dimethylation of these readily available alcohols provide efficient access to this uncommon functional array. In addition, an unusual silane exchange reaction was observed in the reduction of the propargylic alcohols. [ABSTRACT FROM AUTHOR]

Published
2017
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