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

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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.

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Brown, M. F., Marfat, A., Antognoli, G., Chambers, R. J., Cheng, J. B., Damon, D. B., … Watson, J. W. (1998). N-carbamoyl analogs of Zafirlukast: Potent receptor antagonists of leukotriene D4. Bioorganic and Medicinal Chemistry Letters, 8(18), 2451–2456. https://doi.org/10.1016/S0960-894X(98)00442-9

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