93797-48-9Relevant academic research and scientific papers
Octahydropyrazinopyridoindoles. A New Class of Potent Antihypertensive Agents
Jirkovsky, Ivo,Santroch, George,Baudy, Reinhardt,Oshiro, George
, p. 388 - 394 (2007/10/02)
Simplifications and modifications of the vincamine molecule led to the discovery of antihypertensive 1,2,3,4,4a,5,6,12b-octahydro-12-methylpyrazinopyridoindoles.Stereoselective syntheses of both 4a,12b-cis and 4a,12b-trans isomers represent new annulation strategies for the construction of fused piperazines.Compounds of the trans series were at least 10 times more potent than the corresponding cis isomers.Antihypertensive activity and α1-adrenoceptor blocking properties peaked with a simulataneous introduction of 4-methylethyl and 1-alkyl substituents.Compound 15j (AY-28,228: atiprosin), (4a,12b-trans)-1-ethyl- 1,2,3,4,4a,5,6,12b-octahydro-12-methyl-4-(1-methylethyl)pyrazinopyridoindole, was chosen for a detailed preclinical evaluation.
Pyrazino[2',3'-3,4]pyrido[1,2-a]indole derivatives
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, (2008/06/13)
Herein is disclosed pyrazino[2',3'-3,4]pyrido[1,2-a]indole derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.
