메뉴 건너뛰기




Volumn 18, Issue 15, 2008, Pages 4355-4359

Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity

Author keywords

Carbamate; CNS penetration; H bond acceptor capacity; Noradrenaline reuptake inhibitor; NRI

Indexed keywords

AMIDE; ATOMOXETINE; CARBAMIC ACID DERIVATIVE; DOPAMINE; GLYCOPROTEIN P; N (BIPHENYL 2 YLMETHYL)PYRROLIDIN 3 AMINE DERIVATIVE; NORADRENALIN UPTAKE INHIBITOR; PF 3609113; REBOXETINE; SEROTONIN; SULFONAMIDE; UNCLASSIFIED DRUG;

EID: 47749116831     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.06.071     Document Type: Article
Times cited : (14)

References (29)
  • 2
    • 28444469759 scopus 로고    scopus 로고
    • For a recent review of new chemical entities, see:
    • For a recent review of new chemical entities, see:. Walter M.W. Drug Dev. Res. 65 (2005) 97
    • (2005) Drug Dev. Res. , vol.65 , pp. 97
    • Walter, M.W.1
  • 13
    • 47749127772 scopus 로고    scopus 로고
    • Middleton, D. S. Abstracts of Papers, 230th ACS National Meeting, Washington, DC, United States, Aug 28-Sep 1, 2005, MEDI-288.
    • Middleton, D. S. Abstracts of Papers, 230th ACS National Meeting, Washington, DC, United States, Aug 28-Sep 1, 2005, MEDI-288.
  • 14
    • 47749121847 scopus 로고    scopus 로고
    • Whitlock, G. A.; Wakenhut, F.; Stobie, A.; Fish, P. V.; Fray, M. J. Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29, 2007, MEDI-019.
    • Whitlock, G. A.; Wakenhut, F.; Stobie, A.; Fish, P. V.; Fray, M. J. Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29, 2007, MEDI-019.
  • 15
    • 47749155689 scopus 로고    scopus 로고
    • Andrews, M. A; Brown, A. B.; Fish, P. V.; Fray, M. J.; Lansdell, M.; Ryckmans, T.; Stobie, A.; Wakenhut, F.; Whitlock, G. A.; Gray D. L. WO Patent 064351, 2006.
    • Andrews, M. A; Brown, A. B.; Fish, P. V.; Fray, M. J.; Lansdell, M.; Ryckmans, T.; Stobie, A.; Wakenhut, F.; Whitlock, G. A.; Gray D. L. WO Patent 064351, 2006.
  • 17
    • 47749144407 scopus 로고    scopus 로고
    • note
    • 2+) (L-type diltiazem site).
  • 18
    • 35748934487 scopus 로고    scopus 로고
    • Preferred examples in Table 2 had calculated properties for ligand efficiency (LE ≥ 0.45) and ligand-lipophilic efficiency (LLE ≥ 5.0) consistent with drug-like chemical space. For an analysis of drug-like concepts, especially lipophilicity, see:
    • Preferred examples in Table 2 had calculated properties for ligand efficiency (LE ≥ 0.45) and ligand-lipophilic efficiency (LLE ≥ 5.0) consistent with drug-like chemical space. For an analysis of drug-like concepts, especially lipophilicity, see:. Leeson P.D., and Springthorpe B. Nat. Rev. Drug Dis. 6 (2007) 881
    • (2007) Nat. Rev. Drug Dis. , vol.6 , pp. 881
    • Leeson, P.D.1    Springthorpe, B.2
  • 21
    • 47749091337 scopus 로고    scopus 로고
    • note
    • The CNS analysis was limited by an incomplete set of in vivo data and so the correlation was performed against performance in the in vitro MDCK-mdr1 cell line.
  • 22
    • 0032518454 scopus 로고    scopus 로고
    • For a substrate model of the P-gp transporter, see:
    • For a substrate model of the P-gp transporter, see:. Seelig A. Eur. J. Biochem. 251 (1998) 252
    • (1998) Eur. J. Biochem. , vol.251 , pp. 252
    • Seelig, A.1
  • 28
    • 47749098567 scopus 로고    scopus 로고
    • note
    • i = 2.5 nM (n = 2).
  • 29
    • 47749109144 scopus 로고    scopus 로고
    • note
    • +). For 11b D-tartrate salt: mp 117 °C.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.