Design, Synthesis and Evaluation of Novel 4‐(4‐Chlorobenzyl)‐6‐methylpyridazin‐3(2H)‐one Derivatives as Hepatitis B Virus Inhibitors. Issue 40 (21st October 2022)

• Record Type: Journal Article
• Authors: Unsal Tan, Oya; Moncol, Jan; Durantel, David
• Is Part Of: ChemistrySelect. Volume 7:Issue 40(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2022-10-21
• Subjects: Anti-Hepatitis B virus activity -- capsid assembly modulators -- pyridazin-3-one -- synthesis -- x-ray analysis; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.202203164
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: 22 Novel pyridazin‐3‐ones have been designed for anti‐hepatitis B virus (HBV) activity by structural modifications of 3711 which is capsid assembly modulator. Structure of the target compounds were confirmed by elemental analysis and spectroscopic data including X‐ray studies. Among them, the compound having piperazine moiety showed notable inhibitory activity on secretion of HBV DNA and HBeAg which is comparable to that of AT‐130. The preliminary structure‐activity relationships (SARs) of the newly synthesized pyridazin‐3‐one analogues were summarized, which may help researchers to discover more potent anti‐HBV agents bearing pyridazine‐3‐one scaffold. Abstract : 22 Novel pyridazin‐3‐ones have been designed for anti‐hepatitis B virus activity by structural modifications of 3711 which is capsid assembly modulator. Structure of the target compounds were confirmed by elemental analysis and spectroscopic data including X‐ray studies. The compound having piperazine moiety demonstrated the highest in vitro antiviral activity. The molecular modeling analysis was discussed for the most active compound.