A series of 2-cycloalkylamino-3-phenyl-1,8-naphthyridine derivatives, variously substituted in the 6- and 7-positions were synthesized and tested for their ability to inhibit human platelet aggregation in vitro induced by arachidonate, collagen and ADP. Compounds 5a,b, 7a,b, 8a and 10c,d showed a remarkable activity similar to that of indomethacin in the test with arachidonate and collagen. In the test with ADP only compound 8a showed a significant activity. The presence of a morpholinyl or piperidinyl group in position 2 and of a chloro or methoxy group in position 7 of the 1,8-naphthyridine nucleus seem to favour a higher activity. However on the basis of the pharmacological results, no structure-activity relationship can be deduced. Compounds 5b and 7b, which possess the best activity in the arachidonate test, were also shown to increase the c-AMP level significantly, without involving the adenylyl cyclase system.
|Autori:||P.L. FERRARINI; C. MORI; M. BADAWNEH F. FRANCONI; MANERA C; M. MICELI; G. SACCOMANNI|
|Titolo:||Synthesis and antiplatelet activity of some 3-phenyl-1,8-naphthyridine derivatives|
|Anno del prodotto:||2000|
|Digital Object Identifier (DOI):||10.1016/S0014-827X(00)00085-9|
|Appare nelle tipologie:||1.1 Articolo in rivista|