Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India.

Published: March 2013

AI Article Synopsis

  • A new group of compounds featuring a 4,5-dihydro-5-methylisoxazoline structure have been created to act as VLA-4 receptor antagonists.
  • Compound (14p) demonstrated a strong binding affinity to the receptor at 4 nM.
  • Additionally, this compound showed good metabolic stability in laboratory tests.

Article Abstract

A novel set of compounds containing a 4,5-dihydro-5-methylisoxazoline have been successfully designed as VLA-4 receptor antagonists. Compound (14p) had a high receptor binding affinity of 4 nM and also found to be metabolically stable in vitro.

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Source
http://dx.doi.org/10.1016/j.bmcl.2012.12.043DOI Listing

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