[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring

Maosheng Duan, Christopher Aquino, Robert Ferris, Wieslaw M. Kazmierski, Terry Kenakin, Cecilia Koble, Pat Wheelan, Chris Watson, Michael Youngman

Research output: Contribution to journalArticle

  • 18 Citations

Abstract

Several series of CCR5 antagonists have been discovered by derivatization at the N-terminal of the piperidine ring of the core template 2. Some derivatives exhibited potent inhibition against HIV-1infection. The pharmacokinetic properties of the lead compounds 11a, 14a, 15b, and 16b have been evaluated in vivo.

LanguageEnglish (US)
Pages1610-1613
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number6
DOIs
StatePublished - Mar 15 2009
Externally publishedYes

Fingerprint

Lead compounds
Pharmacokinetics
Amines
HIV
Derivatives
piperidine

Keywords

  • Antagonist
  • Antiviral
  • CCR5
  • Derivatization

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists : derivatizations at the N-terminal of the piperidine ring. / Duan, Maosheng; Aquino, Christopher; Ferris, Robert; Kazmierski, Wieslaw M.; Kenakin, Terry; Koble, Cecilia; Wheelan, Pat; Watson, Chris; Youngman, Michael.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 6, 15.03.2009, p. 1610-1613.

Research output: Contribution to journalArticle

Duan, M, Aquino, C, Ferris, R, Kazmierski, WM, Kenakin, T, Koble, C, Wheelan, P, Watson, C & Youngman, M 2009, '[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring' Bioorganic and Medicinal Chemistry Letters, vol 19, no. 6, pp. 1610-1613. DOI: 10.1016/j.bmcl.2009.02.014
Duan, Maosheng ; Aquino, Christopher ; Ferris, Robert ; Kazmierski, Wieslaw M. ; Kenakin, Terry ; Koble, Cecilia ; Wheelan, Pat ; Watson, Chris ; Youngman, Michael. / [2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists : derivatizations at the N-terminal of the piperidine ring. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 6. pp. 1610-1613
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