Histamine H3 receptor is widely expressed in the mammalian brain and is believed to be involved in regulating the release of key neurotransmitters that are involved in attention, vigilance, and cognition. Thus, H3R antagonists may have potential utility in addressing a variety of cognitive and sleep disorders. We have identified a novel series of aryl/heteroaryl amide compounds as highly potent and selective H3 receptor antagonists with a favorable pharmacokinetic properties and no hERG liability. The design, synthesis, SAR and pharmacological profile along with neurochemical profile of these novel compounds for potential treatment of cognitive dysfunction will be presented.

Discovery of novel amides: Highly potent and selective histamine H3 receptor antagonists and their procognitive potential

243rd National Meeting (2012)

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