Microwave accelerated synthesis of isoxazole hydrazide inhibitors of the system xc-rter: Initial homology model

Afnan A. Matti, Joseph Mirzaei, John Rudolph, Stephen A. Smith, Jayme L. Newell, Sarjubhai A. Patel, Michael R. Braden, Richard J. Bridges, Nicholas R. Natale

Research output: Contribution to journalArticlepeer-review

Abstract

Microwave accelerated reaction system (MARS) technology provided a good method to obtain selective and open isoxazole ligands that bind to and inhibit the Sxc- antiporter. The MARS provided numerous advantages, including: shorter time, better yield and higher purity of the product. Of the newly synthesized series of isoxazoles the salicyl hydrazide 6 exhibited the highest level of inhibitory activity in the transport assay. A homology model has been developed to summarize the SAR results to date, and provide a working hypothesis for future studies.

Original languageEnglish
Pages (from-to)5931-5935
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number21
DOIs
StatePublished - Nov 1 2013

Keywords

  • Cystine
  • Glutamate
  • Isoxazole
  • Microwave
  • Transporter

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