| Autor: |
Huang FC; Rhone-Poulenc Rorer Central Research, King of Prussia, Pennsylvania 19406., Galemmo RA Jr, Poli GB, Learn KS, Morrissette MM, Johnson WH Jr, Dankulich WP, Campbell HF, Carnathan GW, VanInwegen RG |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1991 May; Vol. 34 (5), pp. 1704-7. |
| DOI: |
10.1021/jm00109a025 |
| Abstrakt: |
The combination of the benzopyran-4-one ring, a moiety found in the prototype leukotriene antagonist, FPL 55,712, with the (2-quinolinylmethoxy)phenyl group led to a significant increase in leukotriene receptor binding affinity. This modification resulted in a 10,000-fold improvement in binding affinity compared to FPL 55,712. Compound 7 (RG 12553), with a Ki value of 0.1 nM, has higher affinity than the natural agonist LTD4 and is one of the most potent LTD4 antagonists reported. The structure-activity relationships of this series of potent leukotriene antagonists are discussed. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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