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Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists
Authors:Ajay Soni  Abdul Rehman  Keshav Naik  Sunanda Dastidar  MS Alam  Abhijit Ray  Tridib Chaira  Vanya Shah  Venkata P Palle  Ian A Cliffe  Viswajanani J Sattigeri
Institution:1. Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India;2. Department of Pharmacology, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India;3. Department of Chemistry, Jamia Hamdard, New Delhi 110062, India
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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