Pyridazinones and pyrrolones as promising Scaffolds in Medicinal Chemistry

Abstract

Pyridazinones and pyrrolones are important building blocks for some important drugs such as the naturally occurring antibacterial pyrrolone, althiomycin; the cardiotonic pyridazinones, pimobendan and levosimendan and the analgesic anti-inflammatory, emorfozan. Therefore, researchers all over the world paid attention to prepare various pyridazinones and pyrroolones derivatives. The variability in the biological response and ease of preparation from the corresponding furanones attracted attention of researchers to explore these two nuclei in the design and synthesis of different analogues. This review article focuses on different biological activities, structure activity relationship and mechanism of action of pyridazinones and pyrrolones derivatives.

Anti‐inflammatory activity of pyridazinones: A review

“…[38] The oxo derivative of pyridazine that is pyridazin-3(2H)-one scaffold (either saturated or unsaturated) is known as the "wonder nucleus" as it gives out diverse derivatives with all types of pharmacological activities, so it is a vital scaffold in drug discovery and development. [39][40][41][42] This study focuses on the development of pyridazinones as promising anti-inflammatory agents, covering the articles published from 1999 to 2021.…”

“…The oxo derivative of pyridazine that is pyridazin‐3(2 H )‐one scaffold (either saturated or unsaturated) is known as the “wonder nucleus” as it gives out diverse derivatives with all types of pharmacological activities, so it is a vital scaffold in drug discovery and development. [ 39–42 ]…”

Synthesis of Alkyne-Substituted Dihydropyrrolones as Bacterial Quorum-Sensing Inhibitors of Pseudomonas aeruginosa

“…[ 11 , 12 ] Several DHPs were found to possess antimicrobial activity, QS, and biofilm inhibitory activities [ 13 ] such as those reported by our group [ 14 , 15 , 16 ], including DHPs with a thioether [ 17 ] or a seleno-urea [ 18 ] moiety. In addition, the biological activities of DHP-related compounds were also studied by other research groups [ 19 , 20 , 21 , 22 ], including rubrolide derivatives, which showed antibacterial [ 23 ], anticancer [ 24 ], and herbicidal [ 25 ] activities. Moreover, a recent paper by Ma et al also reported the synthesis and anti-virulence activities of several furanones and aryl-substituted pyrrolidone derivatives as quorum sensing inhibitors [ 26 ].…”

Molecular targets and anticancer activity of quinoline–chalcone hybrids: literature review

“…Quinoline derivatives also display excellent anticancer activities via different mechanisms of action, such as the inhibition of tyrosine kinase, alkylating agents, cell cycle arrest, angiogenesis inhibition, apoptosis induction, cell migration disruption, targeting Bcl-2, and inhibition of antimitotic tubulin polymerization [74][75][76][77][78][79][80][81][82][83][84][85][86][87][88] (see ESI †).…”