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Volumn 21, Issue 21, 2011, Pages 6414-6416

Discovery of potent selective orally active benzoxazepine-based orexin-2 receptor antagonists

Author keywords

Insomnia; Orexin 2 receptor antagonists; Sleep disorder

Indexed keywords

DIBENZOXAZEPINE DERIVATIVE; OREXIN 2 RECEPTOR ANTAGONIST; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

EID: 80054788101     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.08.093     Document Type: Article
Times cited : (28)

References (25)
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    • One of examples for quinoid bioactivation is troglitazone as PPAR gamma agonist
    • One of examples for quinoid bioactivation is troglitazone as PPAR gamma agonist. See references
    • See references
  • 15
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    • and references cited therein
    • (b) Ojha, P. K.; Roy, K. Eur. J. Med. Chem. 2010, 45, 4645. and references cited therein..
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    • Ojha, P.K.1    Roy, K.2
  • 16
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    • Guidlines for drug and analogue design
    • Wolff M.E. Ed. Wiley-Interscience: New York
    • Craig, P. N. Guidlines for drug and analogue design. In The Basis of Medicinal Chemistry, vol. 1; Wolff, M. E., Ed.; Wiley-Interscience: New York, 1980. p. 165.
    • (1980) The Basis of Medicinal Chemistry , vol.1 , pp. 165
    • Craig, P.N.1
  • 21
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    • MDR1 directional transport ratio (B to A/A to B) as below 3.0 means low susceptibility of P-gp
    • Passive permeability as over 20 nm/s means high permeability. MDR1 directional transport ratio (B to A/A to B) as below 3.0 means low susceptibility of P-gp.
    • Passive Permeability as Over 20 nm/s means High Permeability
  • 24
    • 34447548576 scopus 로고    scopus 로고
    • Ligand efficiency (LE) is the binding energy per heavy atom (kcal mol-1) = D G/number of heavy atoms =-1.36 log (OX2R IC50)/number of heavy atoms
    • (c) Abad-Zapatero, C. Expert Opin. Drug Discov. 2007, 2, 469. Ligand efficiency (LE) is the binding energy per heavy atom (kcal mol-1) = D G/number of heavy atoms =-1.36 log (OX2R IC50)/number of heavy atoms.
    • (2007) Expert Opin. Drug Discov. , vol.2 , pp. 469
    • Abad-Zapatero, C.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.