Synthesis and in-vitro anti-hepatitis B virus activity of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates

Arch Pharm (Weinheim). 2011 Mar;344(3):158-64. doi: 10.1002/ardp.201000045. Epub 2010 Dec 22.

Abstract

A series of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylate derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in HepG2.2.15 cells. Nearly half of the tested compounds were proved to be highly effective in inhibiting the replication of HBV DNA with IC(50) values ranging from 1.3 to 9.1 µM. Among them, 10o and 10s were identified as the most promising compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Carboxylic Acids / chemical synthesis
  • Carboxylic Acids / chemistry
  • Carboxylic Acids / pharmacology*
  • Cell Line
  • DNA Replication / drug effects
  • DNA, Viral / drug effects
  • Hepatitis B virus / drug effects*
  • Humans
  • Inhibitory Concentration 50
  • Structure-Activity Relationship
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Carboxylic Acids
  • DNA, Viral