The first potent and selective non-imidazole human histamine H4 receptor antagonists.

Jill A Jablonowski, Cheryl A Grice, Wenying Chai, Curt A Dvorak, Jennifer D Venable, Annette K Kwok, Kiev S Ly, Jianmei Wei, Sherry M Baker, Pragnya J Desai, Wen Jiang, Sandy J Wilson, Robin L Thurmond, Lars Karlsson, James P Edwards, Timothy W Lovenberg, Nicholas I Carruthers

Index: J. Med. Chem. 46 , 3957-3960, (2003)

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Abstract

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.