Singulair Structure Activity Relationship, Montelukast Singulair, Bioorg Med Chem Lett, Merck Frosst, Bioorg Med Chem
I had made the point that Merck had looked at structures other than quinolines. I am not making a reference at the time frame just that they looked at other structures. I didn't have the proof of that then so I am posting that now. ... more »
I had made the point that Merck had looked at structures other than quinolines. I am not making a reference at the time frame just that they looked at other structures. I didn't have the proof of that then so I am posting that now.
L-733,321 a pyridyl analog of montelukast was an alternative leukotriene receptor antagonist.( L-733,560 is Merck's anti-fungal drug Cancidas.)
Bioorg Med Chem Lett. 1998 Mar 3;8(5):453-8. Links
A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair
Guay D, Gauthier JY, Dufresne C, Jones TR, McAuliffe M, McFarlane C, Metters KM, Prasit P, Rochette C, Roy P, Sawyer N, Zamboni R.
Merck Frosst Center for Therapeutic Research, Québec, 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.
PMID: 9871597 [PubMed - indexed for MEDLINE]
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