Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework

…, R Rigolio, M Luttmann, V Vecchietti…

文献索引：Giardina, Giuseppe A. M.; Sarau, Henry M.; Farina, Carlo; Medhurst, Andrew D.; Grugni, Mario; Raveglia, Luca F.; Schmidt, Dulcie B.; Rigolio, Roberto; Luttmann, Mark; Vecchietti, Vittorio; Hay, Douglas W. P. Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1794 - 1807

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被引用次数: 81

摘要

A novel class of potent and selective non-peptide neurokinin-3 (NK-3) receptor antagonists, featuring the 4-quinolinecarboxamide framework, has been designed based upon chemically diverse NK-1 receptor antagonists. The novel compounds 33-76, prompted by chemical modifications of the prototype 4, have been characterized by binding analysis using a membrane preparation of chinese hamster ovary (CHO) cells expressing the ...