Antihypertensive 5,6-diarylpyridazin-3-ones

Abstract

The synthesis of a series of 5,6-diarylpyridazinones is described. Some members of this series display an antihypertensive effect in both the spontaneously hypertensive rat (SHR) model and the deoxycorticosteroid (DOCA) model of hypertension. The most potent compounds in the series have halogen substituents on the 5,6-diphenyl rings, a beta-substituted alkyl group at the 2 position of the ring, and acetyl or cyano substituent at the 4 position.

Studies on Some 3(2H)-Pyridazinone Derivatives with Antinociceptive Activity

“…In addition, various compounds incorporating a 3(2H)-pyridazinone ring have been synthesized and their pharmacological activities have been reported [10][11][12] . Recently it was reported that a considerable number of 3(2H)-pyridazinone derivatives have analgesic activity [6,[13][14][15][16][17][18] .…”

Palladium catalyzed reactions on chloropyridazines

“…These pyridazinones are important intermediates in the synthesis of biologically active pyridazines such as the βblocker Prizidilol [4,42,44]. But, also in the class of the pyridazinones themselves a lot of biologically active compounds can be found: 6-aryl-3(2H)-pyridazinones such as the cardiotonic agent Zardaverine [44], analgesic 4,6diaryl-3(2H)-pyridazinones [52], and antihypertensive 5,6diaryl-3(2H)-pyridazinones [53]. To the best of our knowledge in the literature only a few examples of 5-substituted 4-aryl-, 4-substituted 5-aryl-or 4,5-diaryl-3(2H)-pyridazinones can be found [5,[54][55][56][57].…”

(−)-Rhazinilam and the diphenylpyridazinone NSC 613241: Two compounds inducing the formation of morphologically similar tubulin spirals but binding apparently to two distinct sites on tubulin

“…The original DPP compounds were synthesized as antihypertensives [14,15], and some of them had herbicidal activity [16]. In a toxicological study, mitotic figures were found in renal tissue [17,18].…”