Bioorganic & Medicinal Chemistry Letters 2008-07-15

Novel H3 receptor antagonists with improved pharmacokinetic profiles.

Vincent J Santora, Jonathan A Covel, Rena Hayashi, Brian J Hofilena, Jason B Ibarra, Michelle D Pulley, Michael I Weinhouse, Graeme Semple, Albert Ren, Guilherme Pereira, Jeffrey E Edwards, Marissa Suarez, John Frazer, William Thomsen, Erin Hauser, Jodie Lorea, Andrew J Grottick, Vincent J. Santora, Jonathan A. Covel, Rena Hayashi, Brian J. Hofilena, Jason B. Ibarra, Michelle D. Pulley, Michael I. Weinhouse, Graeme Semple, Albert Ren, Guilherme Pereira, Jeffrey E. Edwards, Marissa Suarez, John Frazer, William Thomsen, Erin Hauser, Jodie Lorea, Andrew J. Grottick

文献索引：Bioorg. Med. Chem. Lett. 18(14) , 4133-6, (2008)

全文：HTML全文

摘要

A new series of H(3) antagonists derived from the natural product Conessine are presented. Several compounds from these new series retain the potency and selectivity of earlier diamine based analogs while exhibiting improved PK characteristics. One compound (3u) demonstrated functional antagonism of the H(3) receptor in an in vivo pharmacological model.