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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Matti, Afnan A.^1,2  Mirzaei, Joseph^1,2  Rudolph, John¹  Smith, Stephen A.¹  Newell, Jayme L.¹  Patel, Sarjubhai A.¹  Braden, Michael R.¹  Bridges, Richard J.¹  Natale, Nicholas R.^1,2 

[1] Univ Montana, Ctr Struct & Funct Neurosci, Dept Biomed & Pharmaceut Sci, Missoula, MT 59812 USA

[2] Univ Montana, Med Chem Grad Program, Missoula, MT 59812 USA

关键词: Glutamate;    Cystine;    Transporter;    Isoxazole;    Microwave;   

DOI  :  10.1016/j.bmcl.2013.08.080

来源: Elsevier

【 摘 要 】

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. (C) 2013 Elsevier Ltd. All rights reserved.

【 授权许可】

Free