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.
Gall, M.,McCall, J. M.,TenBrink, R. E.,VonVoigtlander, P. F.,Mohrland, J. S.
p. 1816 - 1820
(2007/10/02)
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