The synthesis of a series of N-substituted O-(3-amino-2-hydroxypropyl)oximes of 1,3,3-trimethyl-5-endo-(1-piperidinyl or 4-morpholinyl)-2-oxabicyclo[2.2.2]octan-6-ones I (NR22 = piperidinylarmopholino, NR21 = NEt2, NHCH2CH2OEt or N-contg. heterocyclic) is described. Some of these ethers showed strong local anesthetic activity in mice and platelet antiaggregating activity in vitro comparable to that of acetylsalicylic acid, as well as moderate hypotensive, antiarrhythmic and analgesic activities in rats and mice.
N-Substituted O-(3-amino-2-hydroxypropyl)oximes of 1,3,3-trimethyl-5-endo-(1-piperidinyl or 4-morpholinyl)-2-oxabicyclo[2.2.2]octan-6-ones with platelet antiaggregating and local anesthetic activities
SCHENONE, SILVIA;BRUNO, OLGA;RANISE, ANGELO;BONDAVALLI, FRANCESCO;
1992-01-01
Abstract
The synthesis of a series of N-substituted O-(3-amino-2-hydroxypropyl)oximes of 1,3,3-trimethyl-5-endo-(1-piperidinyl or 4-morpholinyl)-2-oxabicyclo[2.2.2]octan-6-ones I (NR22 = piperidinylarmopholino, NR21 = NEt2, NHCH2CH2OEt or N-contg. heterocyclic) is described. Some of these ethers showed strong local anesthetic activity in mice and platelet antiaggregating activity in vitro comparable to that of acetylsalicylic acid, as well as moderate hypotensive, antiarrhythmic and analgesic activities in rats and mice.
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