Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists

• Published in: Bioorganic & medicinal chemistry letters Vol. 8; no. 24; pp. 3577 - 3582
• Main Authors: CHAMBERS, R. J, ANTOGNOLI, G. W, CHENG, J. B, KUPERMAN, A. V, LISTON, T. C, MARFAT, A, OWENS, B. S, PILLAR, J. S, SHIRLEY, J. T, WATSON, J. W
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier 15.12.1998
• Subjects: Animals; Anti-Asthmatic Agents - chemical synthesis; Anti-Asthmatic Agents - pharmacokinetics; Anti-Asthmatic Agents - pharmacology; Biological and medical sciences; Biological Availability; Guinea Pigs; Humans; Leukotriene Antagonists; Magnetic Resonance Spectroscopy; Medical sciences; Membrane Proteins; Pharmacology. Drug treatments; Quinolines - chemical synthesis; Quinolines - pharmacokinetics; Quinolines - pharmacology; Rats; Receptors, Leukotriene; Respiratory system; Stereoisomerism; Thiazoles - chemical synthesis; Thiazoles - pharmacokinetics; Thiazoles - pharmacology; U937 Cells; Enantiomer(+); Intravenous administration; Enantioselectivity; Rat; Nitrogen heterocycle; Lung; Leukotriene D4; Antiasthma agent; Oxygen heterocycle; Chroman derivatives; Guinea pig; Structure activity relation; Chlorine Organic compounds; Bicyclic compound; Aromatic compound; Antagonist; Secondary alcohol; Chemical synthesis; Biological receptor; Sulfur nitrogen heterocycle; Rodentia; Benzene derivatives; Quinoline derivatives; Benzothiazole derivatives; In vitro; In vivo; Vertebrata; Mammalia; Animal; Affinity; Fluorine Organic compounds; Pharmacokinetics

A new series of cysLT1 receptor antagonists represented by CP-288,886 (7) and CP-265,298 (8) were developed which are equipotent to clinical cysLT1 receptor antagonists Zafirlukast (1) and Pranlukast (2).