A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

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Guay D, Gauthier JY, Dufresne C, Jones TR, McAuliffe M, McFarlane C, Metters KM, Prasit P, Rochette C, Roy P, Sawyer N, Zamboni R

A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

Bioorg Med Chem Lett. 1998 Mar 3;8(5):453-8.

PubMed ID
9871597 [ View in PubMed
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Abstract

The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singulair) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists including 2ab (L-733,321) as an optimized candidate.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MontelukastCysteinyl leukotriene receptor 1IC 50 (nM)0.78N/AN/ADetails