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ID: ALA1134981

Journal: Bioorg Med Chem Lett

Title: Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.

Authors: Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.

Abstract: The synthesis and biological evaluation of a series of functionalized pyrrolidine- and piperidine-containing analogues of our lead LTA(4) hydrolase inhibitor, SC-57461A, is described. A number of compounds showed excellent potency in our in vitro screens and several demonstrated good oral activity in a mouse ex vivo assay. These efforts led to the identification of SC-56938 (14) as a potent, orally active inhibitor of LTA(4) hydrolase.

CiteXplore: 12419366

DOI: 10.1016/s0960-894x(02)00760-6