Potent, selective MCH-1 receptor antagonists

The design and synthesis of potent and selective indanylmethylpiperidine-based MCHR1 antagonists is reported. This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a s...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-02, Vol.18 (4), p.1402-1406
Hauptverfasser:	Erickson, Shawn D., Banner, Bruce, Berthel, Steven, Conde-Knape, Karin, Falcioni, Fiorenza, Hakimi, Irina, Hennessy, Bernard, Kester, Robert F., Kim, Kyungjin, Ma, Chun, McComas, Warren, Mennona, Francis, Mischke, Steven, Orzechowski, Lucy, Qian, Yimin, Salari, Hamid, Tengi, John, Thakkar, Kshitij, Taub, Rebecca, Tilley, Jefferson W., Wang, Hong
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Amides - pharmacokinetics Amides - pharmacology Animals Antagonist Benzimidazoles - chemistry Benzimidazoles - pharmacokinetics Benzimidazoles - pharmacology Biological and medical sciences Crystallography, X-Ray Hormones. Endocrine system Humans Indans - chemistry Indans - pharmacokinetics Indans - pharmacology Indanylmethyl Kinetics MCHR1 Medical sciences Pharmacology. Drug treatments Piperidines - chemistry Piperidines - pharmacokinetics Piperidines - pharmacology Rats Rats, Sprague-Dawley Receptors, Somatostatin - antagonists & inhibitors Receptors, Somatostatin - chemistry Receptors, Somatostatin - metabolism Selectivity Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The design and synthesis of potent and selective indanylmethylpiperidine-based MCHR1 antagonists is reported. This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity profile appropriate for in vivo efficacy studies and safety.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.01.010