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Synthesis and pharmacological profile of two novel heterocyclic chromanols, CP-80,798 and CP-85,958, as potent LTD4 receptor antagonists

E.G. Andrews,G.W. Antognoli,R. Breslow,M. P. Carta,Thomas J. Carty,R. J. Chambers,John B. Cheng,V. L. Cohan,Judith L. Collins,David B. Damon,J. Delehunt,James F. Eggler,James D. Eskra,K. W. Freiert,Hada William Andrew,A. Marfat,Hiroko Masamune,Lawrence S. Melvin,C. J. Mularski,B. A. Naclerio,C J Pazoles,J.S. Pillar,L.A. Rappach,P. Reiche,Frank W. Rusek,Herbert Sherman,J.T. Shirley,Francis J. Sweeney,Jeanene E. Tickner,J. W. Watson,C.F. Wright

Bioorganic & Medicinal Chemistry Letters（1995）

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摘要
Abstract The development of two novel LTD 4 receptor antagonists as clinical candidates for the treatment of asthma is described. The first generation compound, CP-80,798, was found to be a balanced 5-lipoxygenase inhibitor (5-LOI)/LTD 4 antagonist (LTD 4 -A), while the second generation compound, CP-85,958, is a selective LTD 4 antagonist.
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