Pyridazinone: an important element of pharmacophore possessing broad spectrum of activity

Abstract

In the last few years, the pyridazine derivatives have been found to exhibit a wide range of pharmacological activities. A large number of research articles and patents described them, and several drugs based on its nucleus have come into light. Pyridazinone, a derivative of pyridazine, was initially exploited in search of cardiovascular drugs and for its use in agrochemicals, but later on this nucleus was found to be associated with plethora of activities. In this article, we have reviewed the influence of structural changes on the pharmacodynamic profile of the pyridazinone moiety.

Crystal structure and Hirshfeld surface analysis of ethyl 2-[5-(3-chlorobenzyl)-6-oxo-3-phenyl-1,6-dihydropyridazin-1-yl]acetate

“…The related compound pyridazinone is an important pharmacophore with a wide range of biological applications (Asif, 2015), and its chemistry has been studied for several decades. Pyridazinones are used as scaffolds for potential drug candidates (Dubey & Bhosle, 2015;Thakur et al, 2010) because of their significant potential as antimicrobial (Sö nmez et al, 2006), antidepressant (Boukharsa et al, 2016), anti-inflammatory (Barberot et al, 2018), antihypertensive (Siddiqui et al, 2011), analgesic (Gö kçe et al, 2009), anti-HIV (Livermore et al, 1993), anticonvulsant (Partap et al, 2018;Sharma et al, 2014), cardiotonic (Wang et al, 2008), antihistaminic (Tao et al, 2012), glucan synthase inhibitors (Zhou et al, 2011), phosphodiesterase (PDE) inhibitors (Ochiai et al, 2012) and herbicidal (Asif, 2013) agents. ISSN 2056-9890 In this context and in a continuation of our work in this field (Chkirate et al, 2019a,b;Karrouchi et al, 2015Karrouchi et al, , 2016a, we report herein the synthesis and the molecular and crystal structures of the title pyridazinone derivative, together with its Hirshfeld surface analysis.…”

Crystal structure and Hirshfeld surface analysis of 4-(4-methylbenzyl)-6-phenylpyridazin-3(2H)-one

“…Pyridazinone is an important pharmacophore possessing a wide range of biological applications (Asif, 2014;Akhtar et al, 2016). The chemistry of pyridazinones has been an interesting field of study for decades and this nitrogen heterocycle has become a scaffold of choice for the development of potential drug candidates (Dubey & Bhosle, 2015;Thakur et al, 2010). A review of the literature has revealed that substituted pyridazinones have received a lot of attention in recent years because of their significant potential as antimicrobial (Sö nmez et al, 2006), antidepressant (Boukharsa et al, 2016), antiinflammatory (Barberot et al, 2018), antihypertensive (Siddiqui et al, 2011), analgesic (Gö kçe et al, 2009), anti-HIV (Livermore et al, 1993), anticonvulsant (Partap et al, 2018;Sharma et al, 2014), cardiotonic (Wang et al, 2008), antihistaminic (Tao et al, 2012), glucan synthase inhibitors (Zhou et al, 2011), phosphodiesterase (PDE) inhibitors (Ochiai et al, 2012) and herbicidal agents (Asif, 2013).…”

Crystal structure and Hirshfeld surface analysis of (E)-6-(4-hydroxy-3-methoxystyryl)-4,5-dihydropyridazin-3(2H)-one

“…For decades the chemistry of pyridazinones has been an interesting field. This nitrogen heterocycle became a scaffold of choice for the development of potential drug candidates (Akhtar et al, 2016;Dubey & Bhosle, 2015) because pyridazinone and its substituted derivatives are important pharmacophores possessing many different biological applications (Asif, 2014). Such compounds are used as anti-HIV (Livermore et al, 1993), antimicrobial (Sö nmez et al, 2006), anticonvulsant (Partap et al, 2018), antihypertensive (Siddiqui et al, 2011), antidepressant (Boukharsa et al, 2016), analgesic (Gö kçe et al, 2009), anti-inflammatory (Barberot et al, 2018), antihistaminic (Tao et al 2012), cardiotonic (Wang et al, 2008) and herbicidal agents (Asif, 2013) or as glucan synthase inhibitors (Zhou et al, 2011).…”