SYNTHESIS OF 1,8-NAPHTHYRIDINE DERIVATIVES - POTENTIAL ANTIHYPERTENSIVE AGENTS - PART-VII

A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyri dine derivatives, variously substituted, have been synthesized and pha rmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean art erial pressure (MAP) on spontaneously hypertensive rats. For this seri es of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreo ver, the most active and representative compounds 11b, 12a and 16b wer e investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) E lsevier, Paris.