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

Autor: Jayme L. Newell, Sarjubhai A. Patel, Richard J. Bridges, Joseph Mirzaei, Michael Braden, Nicholas R. Natale, Stephen A. Smith, John Rudolph, Afnan A. Matti
Rok vydání: 2013
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 23:5931-5935
ISSN: 0960-894X
Popis: Microwave accelerated reaction system (MARS) technology provided a good method to obtain selective and open isoxazole ligands that bind to and inhibit the Sx c - 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.
Databáze: OpenAIRE