Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan

…, KJ Merchant, S Sadowski, S Hardwicke…

文献索引：MacLeod, Angus M.; Cascieri, Margaret A.; Merchant, Kevin J.; Sadowski, Sharon; Hardwicke, Sarah; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 6 p. 934 - 941

全文：HTML全文

被引用次数: 30

摘要

The 3, 5-bis (trifluoromethyl) benzyl ester of N-acetyl-L-tryptophan (31, which was derived from the screening lead N-ethyl-L-tryptophan benzyl ester, has been used as a starting point to identify high-affinity substance P receptor antagonists with improved in vivo activity. Altering the ester moiety to an amide or ether led to a substantial loss in binding affinity, but conversion to a ketone provided compounds with affinity comparable to the equivalent ...