In vitro studies on a class of quinoline containing histamine H3 antagonists

A novel series of histamine H3 antagonists containing quinoline core was disclosed. Compound 51 showed 50pM affinity for human histamine H3 in the radio ligand binding assay. A series of quinoline containing histamine H3 antagonists is reported herein. These analogs were synthesized via the Friedlander quinoline synthesis between an aminoaldehyde intermediate and a methyl ketone allowing for a wide diversity of substituents at the 2-position of the quinoline ring.