Replacement of the quinoline system in 2-phenyl-4-quinolinecarboxamide NK-3 receptor antagonists

…, S Cavagnera, A Cerri, E Consolandi, S Gagliardi…

Index: Giardina; Artico; Cavagnera; Cerri; Consolandi; Gagliardi; Graziani; Grugni; Hay; Luttmann; Mena; Raveglia; Rigolio; Sarau; Schmidt; Zanoni; Farina Farmaco, 1999 , vol. 54, # 6 p. 364 - 374

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Citation Number: 22

Abstract

Results from a medicinal chemistry approach aimed at replacing the quinoline ring system in the potent and selective human neurokinin-3 (hNK-3) receptor antagonists 1–4 of general formula I are discussed. The data give further insight upon the potential NK-3 pharmacophore. In particular, it is highlighted that both the benzene-condensed ring and the quinoline nitrogen are crucial determinants for optimal binding affinity to the hNK-3 ...