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Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 10, 2011, Pages 2980-2985

Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists

(5) Perrey, David A a Gilmour, Brian P a Runyon, Scott P a Thomas, Brian F a Zhang, Yanan a

a RTI INTERNATIONAL (United States)

Author keywords

Antagonist; Orexin; SB 334867; Structure activity relationships

Indexed keywords

1 (2 METHYL 6 BENZOXAZOLYL) 3 (1,5 NAPHTHYRIDIN 4 YL)UREA; 1,5 NAPHTHYRIDINE; 2 METHYLBENZOXAZOLE; 4 AMINOPHENYL; BENZOXAZOLE DERIVATIVE; DIARYLUREA DERIVATIVE; NAPHTHYRIDINE DERIVATIVE; OREXIN 1 RECEPTOR; QUINALDINE; UNCLASSIFIED DRUG; UREA DERIVATIVE;

ARTICLE; CALCIUM MOBILIZATION; DRUG ACTIVITY; DRUG SCREENING; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION;

BENZOXAZOLES; DRUG DELIVERY SYSTEMS; LIGANDS; MOLECULAR STRUCTURE; PROTEIN BINDING; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NEUROPEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP; UREA;

EID: 79955569841 PISSN: 0960894X EISSN: None Source Type: Journal
DOI: 10.1016/j.bmcl.2011.03.048 Document Type: Article

Times cited : (18)

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- note
- 1H NMR (CDCl3) δ 0.91 (t, 3H), 1.33 (m, 8H), 3.02 (s, 3H), 3.39 (t, 2H), 6.77 (m, 3H), 7.31 (m, 4H), 8.31 (d, 1H), 8.85 (d, 1H); MS (EI) 395 (M+1).

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- 50. The Ke was calculated from the formula: Ke = [L]/(DR-1), where [L] equals the concentration of test compound in the assay and DR equals the dose ratio (A′/A). The data represent the mean from at least three independent experiments.

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