Arylformamidines with Antinociceptive Properties

Article abstract of DOI:10.1021/jm00117a023

A series of formamidines structurally related to clondine were synthesized and investigated as potential nonopiate analgesics.Several of these compounds showed potent analgesic activity (ED₅₀ on HCl writhing <1.0 mg/kg) with low potential for hypotensive effects.A qualitative description of the structure-activity relationship of this series reveals that the 2,4- and 2,6-dimethylphenyl compounds are more potent analgesics than are the corresponding dichlorophenyl compounds.