| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10598319 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
Abstract
Replacement of the N-butyl side-chain of lead 5-HT4 receptor antagonist 2 with propanesulfonylpiperidinyl, morpholinyl, and piperazinyl groups led to higher affinity analogs 4-6. In vitro drug metabolism screens and cassette pharmacokinetic studies in the dog led to identification of the N-methylpiperazinyl analog (6b), which displayed pharmacokinetic, selectivity, and safety parameters sufficient for advancement to the clinic for the treatment of urinary incontinence.
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Authors
Robin D. Clark, Alam Jahangir, Muzaffar Alam, Cynthia Rocha, Lin Lin, Bodil Bjorner, Khanh Nguyen, Carole Grady, Timothy J. Williams, George Stepan, Hai Ming Tang, Anthony P.D.W. Ford,