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Volumn 19, Issue 18, 2009, Pages 5401-5406

Spiropiperidine CCR5 antagonists

Author keywords

Anti HIV 1; Antiviral; CCR5 antagonist; Chemokine; Spiropiperidine

Indexed keywords

1 OXA 3,9 DIAZASPIRO[5.5]UNDECAN 2 ONE DERIVATIVE; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; PIPERIDINE DERIVATIVE; SPIRO COMPOUND; UNCLASSIFIED DRUG;

EID: 68949105607     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.07.122     Document Type: Article
Times cited : (25)

References (13)
  • 8
    • 68949155054 scopus 로고    scopus 로고
    • For assay protocols see: Melville, C.R.; Rotstein, D. M. WO2008119663.
    • For assay protocols see: Melville, C.R.; Rotstein, D. M. WO2008119663.
  • 9
    • 68949158101 scopus 로고    scopus 로고
    • note
    • The thresholds above which intrinsic mircrosomal clearance values were considered to be high were ≥90 μl/min/mL for RLM and ≥35 μl/min/mL for HLM. These scaled to in vivo clearance values ≥70% of liver blood flow using the well-stirred model. Intrinsic microsomal clearance values corresponding to ≤30% of liver blood flow (≤15 μl/min/mL for RLM and ≤6.5 μl/min/mL for HLM) were considered to be low.
  • 12
    • 68949156076 scopus 로고    scopus 로고
    • note
    • The relatively low exposure observed in rat was due to active transport, in addition to metabolic clearance. Pre-treatment with the P-gp inhibitor elacridar gave higher exposures due to reduced biliary excretion and intestinal secretion. Saturation of transporter effects upon higher dosing also gave improved exposures.
  • 13
    • 68949162758 scopus 로고    scopus 로고
    • For more detailed experimental data, see: US Patent, 176703, Ref. 8
    • For more detailed experimental data, see: Gabriel, S. D.; Rotstein, D. M. US Patent 2005, 176703, Ref. 8.
    • (2005)
    • Gabriel, S.D.1    Rotstein, D.M.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.