Novel Nonopioid Non-Antiinflammatory Analgesics: 3-(Aminoalkyl)- and 3-oxazolopyridin-2(3H)-ones

Article abstract of DOI:10.1021/jm00056a010

A series of 3-(aminoalkyl)- and 3-<(4-aryl-1-piperazinyl)alkyl>oxazolo<4,5-b>pyridin-2(3H)-ones were prepared from their respective oxazolo<4,5-b>pyridin-2(3H)-ones. Several members of this group were found to possess potent analgesic activity in the mouse during a p-phenylquinone writhing induced test. Among them, phenylpiperazine compounds with two-carbon length alkyl chains, 2a and 2b, appeared by high analgesic with little toxicity having neither an antiinflammatory effect nor opioid receptor affinity. The synthesis and structure-affinity relationships for this series are detailed.