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Imidazo[1,5-a]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrimidine derivatives as calcium antagonists

1994; Elsevier BV; Volume: 2; Issue: 5 Linguagem: Inglês

10.1016/s0968-0896(00)82188-4

1464-3391

Ramón Alajarı́n, Juan J. Vaquero, Julio Álvarez‐Buílla, Miguel Fau de Casa-Juana, Carlos Sunkel, Jaime G. Priego, Pilar Gómez‐Sal, Rosario Torres,

Synthesis of heterocyclic compounds

Several bicyclic dihydropyrimidines were synthesized and evaluated for their calcium antagonistic activities by comparison with the usual 1,4-dihydropyridine calcium antagonist reference compound nifedipine. The solid-state structure of the isopropyl 2-methyl-4-(3′-nitrophenyl)-1,4-dihydrobenzo[4,5]imidazo[1,2-alpyrimido-3-carboxylate shows that these compounds can adopt the most important structural features of the 1,4-dihydropyridine and 1,4-dihydropyrimidine calcium channel blockers. The high-potassium depolarized rat aorta assay was used for testing the compounds as calcium channel blockers. Some compounds showed interesting vasorelaxant activity.