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Potent, selective MCH-1 receptor antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Feb 15; Vol. 18 (4), pp. 1402-6. Date of Electronic Publication: 2008 Jan 08. - Publication Year :
- 2008
-
Abstract
- 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.
- Subjects :
- Amides chemistry
Amides pharmacokinetics
Amides pharmacology
Animals
Benzimidazoles chemistry
Benzimidazoles pharmacokinetics
Benzimidazoles pharmacology
Crystallography, X-Ray
Humans
Indans chemistry
Indans pharmacokinetics
Kinetics
Piperidines chemistry
Piperidines pharmacokinetics
Piperidines pharmacology
Rats
Rats, Sprague-Dawley
Receptors, Somatostatin chemistry
Receptors, Somatostatin metabolism
Structure-Activity Relationship
Indans pharmacology
Receptors, Somatostatin antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18243691
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.01.010