Design, Synthesis and Evaluation of Novel 4-(4-Chlorobenzyl)-6-methylpyridazin-3(2H)-one Derivatives as Hepatitis B Virus Inhibitors


ÜNSAL TAN O., Moncol J., Durantel D.

CHEMISTRYSELECT, vol.7, no.40, 2022 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 7 Issue: 40
  • Publication Date: 2022
  • Doi Number: 10.1002/slct.202203164
  • Journal Name: CHEMISTRYSELECT
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
  • Keywords: Anti-Hepatitis B virus activity, capsid assembly modulators, pyridazin-3-one, synthesis, x-ray analysis, NS5B POLYMERASE INHIBITORS, OPTIMIZATION, THIADIAZIN-3'-YL)-5-HYDROXY-2H-PYRIDAZIN-3-ONES, PYRIDAZIN-3(2H)-ONES, REPLICATION
  • Hacettepe University Affiliated: Yes

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.