| 摘要 |
<p>Oxadiazolopyrimidine derivs. of formula (I) and their salts are new. In the formula, R is alkyl, alkoxyalkyl, haloalkyl, aralkyl or aryl; R1 is dialkylamino, 1,2,5,6-tetrahydro-1-pyridyl (opt.4-alkyl substd.), piperidino, azabicyclononyl, azabicyclooctyl, 3-pyrrolin-1-yl, 3-hydroxy-1-piperidinyl or 4-hydroxy-1-piperidinyl, with the proviso that R1 can be unsubstd. 1,2,5,6-tetrahydro-1-pyridyl only when R is haloalkyl, aralkyl or aryl). (I) are vasodilators and/or hypotensives, e.g., giving a 29-32% redn. in systolic pressure and a 13-21% increase in cardiac frequency, both lasting for >24 hrs., at a dose of 10 mg./kg. (p.o., rat). A specific cpd. is ethyl 5-piperidino-2-oxo-2H-1,2,4-oxadiazolo 2,3-a pyrimidine-7-carbama- te. In an example, this is prepd. from diethyl 6-piperidino-2,4-pyrimidine-dicarbamate 3-oxide.</p> |
