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Volumn 20, Issue 10, 2010, Pages 3116-3119

Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists

Author keywords

Anti HIV 1; Antiviral; CCR5 antagonist; Chemokine

Indexed keywords

CHEMOKINE RECEPTOR CCR5 ANTAGONIST; HEXAHYDROPYRROLO[3,4]PYRROLE; MARAVIROC; UNCLASSIFIED DRUG;

EID: 77952099769     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.095     Document Type: Article
Times cited : (10)

References (11)
  • 7
    • 77952099743 scopus 로고    scopus 로고
    • note
    • Briefly, for the antiviral assay, pseudo-type particles were generated by co-transfection of envelope deleted HIV-1 genomic plasmid (derived from pNL4-3) and an envelope expression plasmid carrying viral envelope from NL-Bal into 293T cells. Culture supernatant containing pseudo-typed viruses was harvested after 2 days and used to infect JC53-BL reporter cells. Luciferase reporter gene activity was measured 3 days post-infection. For more detailed assay protocols see: Melville, C.R.; Rotstein, D.M. WO2008119663.
  • 8
    • 77952104669 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.
  • 11
    • 77952106468 scopus 로고    scopus 로고
    • For more detailed experimental information, see: Lee, E.K.; Melville, C. R.; Rotstein, D.M. WO2005121145.
    • For more detailed experimental information, see: Lee, E.K.; Melville, C. R.; Rotstein, D.M. WO2005121145.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.