Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction

Hybridization of the substructures from two types of tachykinin NK1 receptor antagonists 1 and 2 generated a novel series of 3-phenylpiperidine-4-carboxamide derivatives 3. Compound 42 showed high metabolic stability and excellent efficacy in the guinea-pig GR-73637-induced locomotive activity assay...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2012-01, Vol.20 (2), p.962-977
Hauptverfasser:	Shirai, Junya, Sugiyama, Hideyuki, Morimoto, Shinji, Maezaki, Hironobu, Yamamoto, Yasuharu, Okanishi, Satoshi, Kamo, Izumi, Matsumoto, Shiho, Ishigami, Keiko, Inatomi, Nobuhiro, Imanishi, Akio, Kawamoto, Makiko, Tarui, Naoki, Hashimoto, Tadatoshi, Ikeura, Yoshinori
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Phenylpiperidine-4-carboxamide Administration, Oral Amides - chemical synthesis Amides - chemistry Amides - pharmacokinetics Amides - pharmacology Animals antagonists chemistry Cytochrome P-450 CYP3A - metabolism Enzyme Activation - drug effects Guinea Pigs Humans hybridization Microsomes - metabolism Motor Activity - drug effects Neurokinin-1 Receptor Antagonists NK1 receptor oral administration pharmacokinetics Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacokinetics Receptors, Neurokinin-1 - metabolism Receptors, Steroid - metabolism Stereoisomerism Tachykinin
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