Synthesis and antihypertensive activity of new 6-heteroaryl-3-hydrazinopyridazine derivatives
- 31 December 1980
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 24 (1) , 59-63
- https://doi.org/10.1021/jm00133a013
Abstract
The synthesis and pharmacological activity of new 6-heteroaryl-3-hydrazinopyridazines with antihypertensive action are described. The introduction of pyrrole, pyrazole, imidazole, triazole, tetrazole, thiophene, indole and carbazole heterocyclic rings into the 6 position of the pyridazine nucleus was carried out by 3 different methods of synthesis. The hypotensive action was examined on normotensive and spontaneously hypertensive rats by comparison with dihydralazine (I). 6-Imidazol-1-yl derivatives proved to be particularly active. Of these derivatives, 3-hydrazino-6-(2-methylimidazol-1-yl)pyridazine (7c) achieves 4.9 times the activity of dihydralazine when administered orally to spontaneously hypertensive rats. The LD50 values of 7c and dihydralazine are very similar.This publication has 1 reference indexed in Scilit:
- Synthesis and antihypertensive activity of novel 3-hydrazino-5-phenyl-1,2,4-triazinesJournal of Medicinal Chemistry, 1979