Synthesis and antirhinovirus activity of 8-substituted analogs of 6-(dimethylamino)-9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine

Several 8-substituted analogues of 6-(dimethylamino) -9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine (1) were synthesized and tested for activity against rhinovirus type 1B. Among 16 8-substituted analogues, the 8-amino (3) and 8-bromo (2) analogues were most active with IC50s of 0.36 and 1.4 micr...

Full description

Saved in:
Bibliographic Details
Published inJournal of medicinal chemistry Vol. 34; no. 1; pp. 157 - 160
Main Authors Kelley, James L, Linn, James A, Selway, J. W. T
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 01.01.1991
Subjects
Antiviral Agents - chemical synthesis
HeLa Cells
Humans
Indicators and Reagents
Magnetic Resonance Spectroscopy
Mass Spectrometry
Molecular Structure
Purines - chemical synthesis
Purines - chemistry
Purines - pharmacology
rhinovirus
Rhinovirus - drug effects
Structure-Activity Relationship
Online AccessGet full text

Cover

More Information
Summary:Several 8-substituted analogues of 6-(dimethylamino) -9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine (1) were synthesized and tested for activity against rhinovirus type 1B. Among 16 8-substituted analogues, the 8-amino (3) and 8-bromo (2) analogues were most active with IC50s of 0.36 and 1.4 microM, respectively, under conditions where 1 had an IC50 of 0.03 microM.
Bibliography:istex:142AE356688FE2231356C510B609A3A8B43CCDBE
ark:/67375/TPS-2R8DGNL0-F
ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
content type line 23
ObjectType-Article-1
ObjectType-Feature-2
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00105a023