Modulation on C??and N??Terminal Moieties of a Series of Potent and Selective Linear Tachykinin NK2 Receptor Antagonists

…, M Altamura, T Dimoulas, V Fedi, D Giannotti…

文献索引：Gensini, Martina; Altamura, Maria; Dimoulas, Tula; Fedi, Valentina; Giannotti, Danilo; Giuliani, Sandro; Guidi, Antonio; Harmat, Nicholas J. S.; Meini, Stefania; Nannicini, Rossano; Pasqui, Franco; Tramontana, Manuela; Triolo, Antonio; Maggi, Carlo Alberto ChemMedChem, 2010 , vol. 5, # 1 p. 65 - 78

全文：HTML全文

被引用次数: 5

摘要

Abstract Herein we describe the synthesis of a series of new potent tachykinin NK 2 receptor antagonists by the modulation of the C-and N-terminal moieties of ibodutant (MEN 15596, 1). The N-terminal benzo [b] thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK 2 ...