N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4.

Article Details

Citation

Brown MF, Marfat A, Antognoli G, Chambers RJ, Cheng JB, Damon DB, Liston TE, McGlynn MA, O'Sullivan SP, Owens BS, Pillar JS, Shirley JT, Watson JW

N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4.

Bioorg Med Chem Lett. 1998 Sep 22;8(18):2451-6.

PubMed ID
9873560 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ZafirlukastCysteinyl leukotriene receptor 1IC 50 (nM)2N/AN/ADetails