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Volumn 20, Issue 14, 2010, Pages 4215-4218

Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses

Author keywords

Aminopyrimidine; Antiviral; HIV; Inhibitor; NNRTI; Reverse transcriptase; Viral mutants

Indexed keywords

BENZOPHENONE DERIVATIVE; BENZYL DERIVATIVE; ETRAVIRINE; GW 678248; GW 69564; PIPERIDINE; PYRIMIDINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 77953872635     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.05.040     Document Type: Article
Times cited : (67)

References (17)
  • 12
    • 77953871966 scopus 로고    scopus 로고
    • note
    • Atomic coordinates for the structures of Etravirine and 5h bound to HIV/RT have been deposited with the RCSB Protein Data Bank (PDB) under the access codes 3M8P, and 3M8Q, respectively.
  • 13
    • 77953869982 scopus 로고    scopus 로고
    • note
    • 50 values were obtained from a SPA heteropolymeric assay. RNA-dependent DNA polymerase activity was measured using a biotinylated primer oligonucleotide and tritiated dNTP substrate. Newly synthesized DNA was quantified by capturing the biotinylated primer molecules on streptavidin coated Scintillation Proximity Assay (SPA) beads (Amersham).
  • 14
    • 77953870422 scopus 로고    scopus 로고
    • For a detailed description of the syntheses of aminopyrimidine inhibitors see: Kertesz, D. J.; Brotherton-Pleiss, C.; Yang, M. US 2008/0146595.
    • For a detailed description of the syntheses of aminopyrimidine inhibitors see: Kertesz, D. J.; Brotherton-Pleiss, C.; Yang, M. US 2008/0146595.
  • 15
    • 0023277417 scopus 로고
    • 50 values were obtained following incubation of compound with infected MT4 cells in the presence of 10% fetal bovine serum (FBS). The assay assesses the reduction in the cytopathic effect of HIV-1 on MT4 cells in the presence of HIV-RT inhibitors. Each value represents the average of at least two independent assays. For a detailed description of the anitiviral assay see:
    • 50 values were obtained following incubation of compound with infected MT4 cells in the presence of 10% fetal bovine serum (FBS). The assay assesses the reduction in the cytopathic effect of HIV-1 on MT4 cells in the presence of HIV-RT inhibitors. Each value represents the average of at least two independent assays. For a detailed description of the anitiviral assay see:. Pauwels R., De C.E., Desmyter J., Balzarini J., Goubau P., Herdewijn P., Vanderhaeghe H., and Vandeputte M. J. Virol. Methods 16 (1987) 171
    • (1987) J. Virol. Methods , vol.16 , pp. 171
    • Pauwels, R.1    De, C.E.2    Desmyter, J.3    Balzarini, J.4    Goubau, P.5    Herdewijn, P.6    Vanderhaeghe, H.7    Vandeputte, M.8
  • 17
    • 77953871573 scopus 로고    scopus 로고
    • note
    • Determination of potency versus wild type virus was repeated in the presence of 40% human serum (HS) for these compounds. The resulting 'protein shifted potency' as compared to the result with 10% FBS (see Ref. 15) is considered an indicator of potential for in vivo activity.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.