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Can I read Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers on EtoBox?
Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers by Lars J.S. Knutsen; Christopher J. Hobbs; Christopher G. Earnshaw; Andrea Fiumana; Jenny Gilbert; Sarah L. Mellor; Fleur Radford; Nichola J. Smith; Philip J. Birch; J. Russell Burley; Stuart D.C. Ward; Iain F. James is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers about?
A series of new N-type (Ca v 2.2) calcium channel blockers derived from the 'hit' structures 2-(3-bromo-4-fluorophenyl)-3-(2-pyridin-2-ylethyl)thiazolidin-4-one 9 and its 2-[4-(4-bromophenyl)pyridin-3-yl]-3-isobutyl analogue 10 is described. Extensive SAR studies using a range of synthetic approaches resulted in novel, patented compounds with IC 50 values of up to 0.2 lM in an in vitro IMR32 assay, and selectivities for N/L of up to 30-fold. The new compounds described have potential in treatment of neuropathic pain.
Who reads Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Lars J.S. Knutsen; Christopher J. Hobbs; Christopher G. Earnshaw; Andrea Fiumana; Jenny Gilbert; Sarah L. Mellor; Fleur Radford; Nichola J. Smith; Philip J. Birch; J. Russell Burley; Stuart D.C. Ward; Iain F. James
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)