合成和评价 4,5-二氢-5-甲基异恶唑啉-5-甲酰胺衍生物作为 VLA-4 拮抗剂。
Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists.
机构信息
Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India.
出版信息
Bioorg Med Chem Lett. 2013 Mar 1;23(5):1482-5. doi: 10.1016/j.bmcl.2012.12.043. Epub 2012 Dec 21.
PMID:23312947
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.
摘要
一组新型的含有 4,5-二氢-5-甲基异恶唑啉的化合物已成功设计为 VLA-4 受体拮抗剂。化合物 (14p) 具有 4 nM 的高受体结合亲和力，并且在体外也发现具有代谢稳定性。
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