A series of formamidines structurally related to clonidine were synthesized and investigated as potential nonopiate analgesics. Several of these compounds showed potent analgesic activity (ED50 on HCl writhing less than 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.;VON, VOIGTLANDER P. F.;MOHRLAND, J+, J. MED. CHEM., 31,(1988) N 9, C. 1816-1820
作者:GALL, M.、MCCALL, J. M.、TENBRINK, R. E.、VON, VOIGTLANDER P. F.、MOHRLAND, J+
DOI:——
日期:——
US4413013A
申请人:——
公开号:US4413013A
公开(公告)日:1983-11-01
Arylformamidines with antinociceptive properties
作者:M. Gall、J. M. McCall、R. E. TenBrink、P. F. VonVoigtlander、J. S. Mohrland
DOI:10.1021/jm00117a023
日期:1988.9
A series of formamidines structurally related to clonidine were synthesized and investigated as potential nonopiate analgesics. Several of these compounds showed potent analgesic activity (ED50 on HCl writhing less than 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.