Structure-activity profile of substituted purines and inflammation in the delayed hypersensitivity skin reaction |
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Authors: | R. J. Wojnar K. A. Losee R. J. Brittain |
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Affiliation: | 1. Department of Biochemical Pharmacology, The Squibb Institute for Medical Research, 08540, Princeton, New Jersey, USA
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Abstract: | Substituted purines were tested for their effectiveness in inhibiting the delayed hypersensitivity skin reaction (DHSR) caused by tuberculin in the guinea-pig. Among the tested purines were naturally occurring derivatives of guanine and adenine, including cyclic AMP. Based on the structure-activity profile, a class of purines was identified, the members of which were very effective inhibitors of inflammatory aspects of the DHSR and are characterized by a benzyl group in position 9, an amino or alkylamino group in position 6, and various substituents in position 2. This class of 2-substituted-9-benzyladenines was more effective in the DHSR than some antimetabolites, particularly the structurally related mercaptopurines. |
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