Studies on Antiulcer Drugs. V. Synthesis and Antiulcer Activity of Aralkylbenzazoles

Abstract

A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H₂-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H₂-receptor antagonist activity in contrast to imidazo[1, 2-α]pyridine analogues (I). On antiulcer assay, however, some pyridine derivatives (II) exerted higher activity than the reference compounds, sofalcone, sucralfate and cimetidine. The structure-activity relationships of these compounds are discussed.