N-carbamoyl analogs of zafirlukast: Potent receptor antagonists of leukotriene D4

Exploration of the indole nitrogen region of Zafirlukast (1) has uncovered a potent series of cysteinyl leukotriene D4 (LTD4) antagonists. These studies showed that a variety of functionality could be incorporated in this region of the molecule without sacrificing potency. Efforts to exploit this si...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-09, Vol.8 (18), p.2451-2456
Hauptverfasser:	BROWN, M. F, MARFAT, A, PILLAR, J. S, SHIRLEY, J. T, WATSON, J. W, ANTOGNOLI, G, CHAMBERS, R. J, CHENG, J. B, DAMON, D. B, LISTON, T. E, MCGLYNN, M. A, O'SULLIVAN, S. P, OWENS, B. S
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Guinea Pigs Haplorhini Humans Leukotriene Antagonists - chemical synthesis Leukotriene Antagonists - pharmacology Medical sciences Membrane Proteins Models, Chemical Pharmacology. Drug treatments Rats Receptors, Leukotriene Respiratory system Tosyl Compounds - chemistry Tosyl Compounds - pharmacology
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Zusammenfassung:	Exploration of the indole nitrogen region of Zafirlukast (1) has uncovered a potent series of cysteinyl leukotriene D4 (LTD4) antagonists. These studies showed that a variety of functionality could be incorporated in this region of the molecule without sacrificing potency. Efforts to exploit this site in order to improve oral efficacy are discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00442-9