| Title : Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase - Penning_2002_Bioorg.Med.Chem.Lett_12_3383 |
| Author(s) : 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 12 :3383 , 2002 |
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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. |
| PubMedSearch : Penning_2002_Bioorg.Med.Chem.Lett_12_3383 |
| PubMedID: 12419366 |
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 (2002)
Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase
Bioorganic & Medicinal Chemistry Lett
12 :3383
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 (2002)
Bioorganic & Medicinal Chemistry Lett
12 :3383