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Bioorg Med Chem Lett ; 12(11): 1533-5, 2002 Jun 03.
Article in English | MEDLINE | ID: mdl-12031336

ABSTRACT

A series of phthalimide acid derivatives was synthesized and evaluated as leukotriene D(4) receptor antagonists. The tetrazolephthalimide LASSBio 552 (7) was shown to be able to inhibit the contractile activity induced by 100 nM of LTD(4) in guinea-pig tracheal strips with an IC(50) = 31.2 microM. In addition, LASSBio 552 (7) has been showed to present a better efficacy than zafirlukast (1) used as standard.


Subject(s)
Anti-Asthmatic Agents/chemical synthesis , Anti-Asthmatic Agents/pharmacology , Leukotriene Antagonists , Membrane Proteins , Phthalimides/chemical synthesis , Phthalimides/pharmacology , Animals , Anti-Asthmatic Agents/chemistry , Drug Design , Guinea Pigs , In Vitro Techniques , Indoles , Models, Molecular , Molecular Conformation , Muscle Contraction/drug effects , Phenylcarbamates , Phthalimides/chemistry , Receptors, Leukotriene/chemistry , Sulfonamides , Tetrazoles/chemistry , Tosyl Compounds/pharmacology , Trachea/drug effects , Trachea/physiology
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