Novel phthalimide derivatives, designed as leukotriene D(4) receptor antagonists

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. I...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-06, Vol.12 (11), p.1533-1535
Main Authors: Lima, Lídia M, de Brito, Fernanda C F, de Souza, Simone D, Miranda, Ana L P, Rodrigues, Carlos R, Fraga, Carlos A M, Barreiro, Eliezer J
Format: Article
Language:English
Subjects:
Animals
Anti-Asthmatic Agents - chemical synthesis
Anti-Asthmatic Agents - chemistry
Anti-Asthmatic Agents - pharmacology
Drug Design
Guinea Pigs
In Vitro Techniques
Leukotriene Antagonists
Membrane Proteins
Models, Molecular
Molecular Conformation
Muscle Contraction - drug effects
Phthalimides - chemical synthesis
Phthalimides - chemistry
Phthalimides - pharmacology
Receptors, Leukotriene - chemistry
Tetrazoles - chemistry
Tosyl Compounds - pharmacology
Trachea - drug effects
Trachea - physiology
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Summary: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.
ISSN:0960-894X