New platelet aggregation inhibitors based on pyridazinone moiety

Polymorphism of 2-(5-benzyl-6-oxo-3-phenyl-1,6-dihydropyridazin-1-yl)acetic acid with two monoclinic modifications: crystal structures and Hirshfeld surface analyses

“…Pyridazin-3(2H)-ones are an important family of heterocycles because of their great chemical reactivity (Chelfi et al, 2015;Zarrouk et al, 2010), with new products reported recently (Chakraborty et al, 2018;El Kalai et al, 2019a). In addition, the importance of pyridazinones in medicinal chemistry has increased in recent years thanks to their pharmacological properties, including anticancer (Yarden & Caldes, 2013), antihypertensive (Siddiqui et al, 2011), antibacterial (Akhtar et al, 2016), anti-HIV (Livermore et al, 1993), anti-inflammatory (Singh et al, 2017), antidepressant (Boukharsa et al, 2016), anti-convulsant (Partap et al, 2018) and cardiotonic (Costas et al, 2015) activities. Several pyridazinone-based products are already present in the pharmaceutical market such as Minaprine (Sotelo et al, 2003), Azanrinone (Mahmoodi et al, 2014), Indolidan (Abouzid et al, 2008) and Levosimendan (Archan & Toller, 2008).…”

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

“…The synthesized compounds were tested in vitro as antiplatelet agents and some of them exhibited potent inhibitory effects on collagen-induced platelet aggregation with IC50 values in the low μM range. The most active compound of these series demonstrated its lack of activity as inhibitor of platelet aggregation induced by other agonists as thrombin, ionomycin or U-46619 suggesting a selective action on the biochemical mechanisms triggered by collagen in the platelets (Costas at al., 2015). In a highthroughput screening campaign for c-Met kinase inhibitors, a thiadiazinone derivative with a carbamate group was identified as a potent in vitro inhibitor.…”

Synthesis, spectroscopy, crystal structure, TGA/DTA study, DFT and molecular docking investigations of (E)-4-(4-methylbenzyl)-6-styrylpyridazin-3(2H)-one

“…They occupy a very important place in heterocyclic chemistry due to their great chemical reactivity [1] allowing access to a multitude of new products of this family [ 2 , 3 ]. Besides, to their chemical reactivity, the place of pyridazinones in medicinal chemistry has not ceased to increase in recent years, due to their wide range of products with interesting pharmacological activities such as anticancer, anti-hypertensive, antibacterial, anti-HIV, antinociceptive, anti-inflammatory, antidepressants, anti-convulsant, cardiotonic and diuretics [4] , [5] , [6] , [7] , [8] , [9] , [10] , [11] , [12] . Moreover, several pyridazinone-based products are already present in the pharmaceutical market such as Minaprine, Azanrinone, Emorfazone, Indolidan, Levosimendan, Primobendan, and Bemoradan [13] , [14] , [15] , [16] , [17] , [18] , [19] ( Fig.…”