Pyrimidine containing RSV fusion inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 2, 2005, Pages 427-430

  Nikitenko, Antonia ^a   Raifeld, Yuri ^a   Mitsner, Boris ^a   Newman, Howard ^a  

^a PFIZER INC   (United States)

Author keywords

Fusion inhibition; Nucleophilic substitution; Respiratory syncytial virus; Trichloropyrimidine

Indexed keywords

PYRIMIDINE DERIVATIVE; TRIAZINE DERIVATIVE;

ANTIVIRAL ACTIVITY; ARTICLE; COMPARATIVE STUDY; DRUG SCREENING; DRUG SYNTHESIS; RESPIRATORY SYNCYTIAL PNEUMOVIRUS;

ANIMALS; ANTIVIRAL AGENTS; PYRIMIDINES; RESPIRATORY SYNCYTIAL VIRUSES; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZINES;

RESPIRATORY SYNCYTIAL VIRUS; RICE STRIPE VIRUS;

EID: 10644297146     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.10.056     Document Type: Article

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15. The reaction intermediates and products were analyzed by reversed-phase HPLC (column: C30-ProntoSIL, 3μ, 2 × 150 mm; mobile phase: A-water, B-acetonitrile, C-methanol; gradient from the mixture A:B:C 88:6:6 v/v to the mixture A:B:C 60:25:15. Preparative reversed-phase HPLC was performed on a Rainin gradient HPLC system using a YMC-Pack Polymer C18, S-10, 20 × 250 mm; mobile phase: A-0.05 M ammonium acetate in water (pH 4.5), B-acetonitrile; isocratic mixture A:B 59:41 v/v, then gradient to the mixture A:B 41:85 v/v in 4 min. Desalting was performed on YMC Prodigy C18 Polymer column, using acetonitrile/water 1:1 mixture
16. 2)
17. 50 values were determined against RSV A2, HCMV AD169 and HSV Patton strains. The RSV and HSV-1 assays are ELISA based; the HCMV assay is via an indicative gene in the virus. Details of the antiviral assays are published in Ref. 7