P. L. Ferrarini

Synthesis and β-blocking activity of (E)- and (Z)-iminoethers of 1,8-naphthyridine. Potential antihypertensive agents. 4

Abstract A series of substituted (E)-and (Z)-iminoethers of 1,8-naphthyridine was synthesized from corresponding ketones. The pharmacological activity of these compounds was evaluated on isolated preparations to assess the eventual interaction with α and β adrenoceptors. All the compounds exhibited β2 stimulating and β1 blocking properties, while on α receptors neither stimulating nor blocking activity was observed.

Synthesis and antiplatelet activity of some 1,8-naphthyridine derivatives

Abstract A series of 1,8-naphthyridine derivatives was synthesized and tested for their ability to inhibit human platelet aggregation in vitro induced by arachidonic acid, collagen and ADP. Some compounds showed remarkable activity and the most active derivatives were comparable to papaverine in the test with arachidonic acid and collagen. In the test with ADP the tested compounds showed no significant activity. The tested compounds that possessed the best activity were also demonstrated to increase the c-AMP level significantly without involving the adenylyl cyclase system.

BROMO DERIVATIVES OF GRAMINES. PREPARATION AND PHARMACOLOGICAL PROPERTIES

Bromieten von Gramin (I) ergibt ein nicht trennbares Gemisch des 5-Bromderivates (II) mit demo-Bromderivat (III), das durch Mannich-Reaktion aus 6-Bromindol (IV) rein . erhalten wird.