| Autor: |
Gapinski DM; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285., Mallett BE, Froelich LL, Jackson WT |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1990 Oct; Vol. 33 (10), pp. 2798-807. |
| DOI: |
10.1021/jm00172a019 |
| Abstrakt: |
A series of lipophilic benzophenone dicarboxylic acid derivatives was prepared which inhibited the binding of the potent chemotaxin leukotriene B4 to its receptor(s) on intact human neutrophils. With a radioligand-binding assay as a measure of receptor affinity, a structure-activity relationship for this series was investigated. Both acidic residues were required for receptor-binding activity. The relative orientation of the two acidic groups was important for optimal binding. Replacement of the carbonyl group of the benzophenone with a variety of polar and nonpolar linking groups led to only small changes in binding affinity, indicating the linking group may not be involved in receptor recognition. Further structure-activity relationships within this series are reported in an accompanying paper. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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