Axially chiral 1, 7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK1 receptor antagonists: synthesis, antagonistic activity, and effects on bladder …

H Natsugari, Y Ikeura, I Kamo, T Ishimaru…

Index: Natsugari, Hideaki; Ikeura, Yoshinori; Kamo, Izumi; Ishimaru, Takenori; Ishichi, Yuji; Fujishima, Akira; Tanaka, Toshimasa; Kasahara, Fumiko; Kawada, Mitsuru; Doi, Takayuki Journal of Medicinal Chemistry, 1999 , vol. 42, # 19 p. 3982 - 3993

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Citation Number: 85

Abstract

Cyclic analogues of N-[3, 5-bis (trifluoromethyl) benzyl]-7, 8-dihydro-N, 7-dimethyl-5-(4- methylphenyl)-8-oxo-1, 7-naphthyridine-6-carboxamide (1) having a 6-9-membered ring (6- 9) were synthesized and evaluated for NK1 antagonistic activities. The 8-membered ring compound with a β-methyl group at the C (9)-position,(aR, 9 R)-7-[3, 5-bis (trifluoromethyl) benzyl]-8, 9, 10, 11-tetrahydro-9-methyl-5-(4-methylphenyl)-7 H-[1, 4] diazocino [2, 1-g][1, ...