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Novel phthalimide derivatives, designed as leukotriene D(4) receptor antagonists
Lídia M Lima1, Fernanda C F de Brito, Simone D de Souza
1LASSBio, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, PO Box 68006, Rio de Janeiro, 21944-970, Brazil.
Bioorganic & Medicinal Chemistry Letters
|May 29, 2002
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.