Novel derivatives of 1, 8-naphthyridine were synthesized from 7-amino-2-hydroxy-4-morpholinomethyl-1, 8-naphthyridine. The ability of the synthesized compounds to inhibit isoproterenol(ISO)-induced phosphorylation of phospholamban (PLB) was assessed. Their ability to block both beta(1) and beta(2) receptors almost completely abolished all ISO effects on phosphorylation of PLB. Analogues with either a 7-hydroxy-2-N-ethoxycarbonylpiperazine or a 7-hydroxy-2-piperazine substituent, designated as 6 and 9 respectively, showed a higher affinity for beta(1) receptor than that of the methoxy derivatives 12 and 13. However, treatment with 30 microM 9 and 1mM 13 lead to comparable levels of PLB phosphorylation. The reduction to 6-amino derivatives 10 and 17 led to compounds possessing beta(2) receptor blocking properties. The ability of the synthesized compounds to inhibit forskolin-stimulated cAMP production was also studied. Together, these results suggest that the 1, 8-naphthyridine parent structure can be modified, to produce compounds with increased activity whose effect in rat appears to be more clearly related to antagonism of beta(1)-rather than beta(2)-adrenergic receptors.
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