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

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

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  • 1Merck Frosst Center for Therapeutic Research, Qu├ębec, Canada.


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.

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