KELLEY, JAMES L.;LINN, JAMES A.;RIDEOUT, JANET L.;SOROKO, FRANCIS E., J. HETEROCYCL. CHEM., 25,(1988) N 4, C. 1255-1258
作者:KELLEY, JAMES L.、LINN, JAMES A.、RIDEOUT, JANET L.、SOROKO, FRANCIS E.
DOI:——
日期:——
Synthesis and anticonvulsant activity of 1-benzyl-4-alkylamino-1<i>H</i>-imidazo[4,5-<i>c</i>]pyridines
作者:James L. Kelley、James A. Linn、Janet L. Hideout、Francis E. Soroko
DOI:10.1002/jhet.5570250441
日期:1988.7
Four 3-deaza analogues of the potent anticonvulsant purine, BW A78U, were synthesized and tested for anticonvulsant activity. The imidazo[4,5-c]pyridines 9–12 were prepared in two steps from 4-chloro-1H-imidazo[4,5-c]pyridine (2). The compounds were potent anticonvulsant agents against maximal electroshock-induced seizures in rats with i.p. ED50 ranging from 2 to 3.5 mg/kg. However, these 3-deazapurines
合成了强抗惊厥嘌呤的四个3-deaza类似物BW A78U,并测试了其抗惊厥活性。咪唑并[4,5-c]吡啶9-12分两步从4-氯-1 H-咪唑并[4,5- c ]吡啶(2)制备。该化合物是有效的抗惊厥药,可对抗ip ED 50为2至3.5 mg / kg的大鼠最大的电击诱发的癫痫发作。但是,这些3-deazapurines的毒性明显高于BW A78U,这使其无法开发为潜在的抗癫痫药。