Tricyclic imidazole antagonists of the Neuropeptide S Receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 15, 2010, Pages 4704-4708

  Trotter, B Wesley ^a   Nanda, Kausik K ^a   Manley, Peter J ^a   Uebele, Victor N ^a   Condra, Cindra L ^a   Gotter, Anthony L ^a   Menzel, Karsten ^a   Henault, Martin ^b   Stocco, Rino ^b   Renger, John J ^a   Hartman, George D ^a   Bilodeau, Mark T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Merck Canada   (Canada)

Author keywords

Neuropeptide S Receptor

Indexed keywords

NEUROPEPTIDE RECEPTOR; NEUROPEPTIDE S; RECEPTOR BLOCKING AGENT;

ARTICLE; CENTRAL NERVOUS SYSTEM; IN VIVO STUDY; NONHUMAN; RAT; SCREENING;

ANIMALS; HETEROCYCLIC COMPOUNDS, 3-RING; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; IMIDAZOLES; RATS; RECEPTORS, NEUROPEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77955413090     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.016     Document Type: Article

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14. Except where noted, compounds were synthesized and tested in racemic form.
15. Except where noted, compounds were synthesized from racemic acids of type 7. Stereogenic amines were also introduced as racemates to afford diastereomeric mixtures; in order to accelerate screening, diastereomers were not separated.
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18. 2 (15:85, 70 mL/min), retention time 5.2 min (faster eluting peak). Absolute stereochemistry has not been determined.
19. An HPLC log D of 3.2 was measured for 15.
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