[摘要]:The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H-3 antagonists is described. Introduction of substituted phenyl, pyridyl and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H-3 antagonist activity in both ex vivo and in vivo assays. (C) 2012 Elsevier Ltd. All rights reserved.