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Discovery Of L-740,515, A Potent Thienopyridine Cyslt(1) Receptor (Ltd(4) Receptor) Antagonist

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(1995)

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Abstract
Structure-activity studies leading to the discovery of a new series of non-quinoline cysLT(1) receptor (LTD(4) receptor) antagonists are described. These studies demonstrated that the quinoline ring system of montelukast(5) may be replaced by an appropriately substituted thienopyridine system, yielding potent compounds. Two other molecular features of montelukast, the terminal phenyl ring substitution and the vinyl link, were also reevaluated. These studies led to the identification of 1 (L-740,515), a compound with optimized in vitro and in vivo biological profiles.
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potent thienopyridine,ltd4 receptor,antagonist,cheminform abstract
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