Synthesis of 2-methoxybenzoylhydrazone and evaluation of their antileishmanial activity

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3463-6. doi: 10.1016/j.bmcl.2013.03.051. Epub 2013 Mar 31.

Abstract

Compounds 1-25 showed varying degree of antileishmanial activities with IC50 values ranging between 1.95 and 88.56 μM. Compounds 2, 10, and 11 (IC50=3.29±0.07 μM, 1.95±0.04 μM, and 2.49±0.03 μM, respectively) were found to be more active than standard pentamidine (IC50=5.09±0.04 μM). Compounds 7 (IC50=7.64±0.1 μM), 8 (IC50=13.17±0.46 μM), 18 (IC50=13.15±0.02 μM), and 24 (IC50=15.65±0.41 μM) exhibited good activities. Compounds 1, 3, 4, 5, 9, 12, 15, 18, and 19 were found to be moderately active. Compounds 13, 14, 16, 17, 20-25 showed weak activities with IC50 values ranging between 57 and 88 μM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology
  • Drug Evaluation, Preclinical
  • Hydrazones / chemical synthesis
  • Hydrazones / chemistry*
  • Hydrazones / pharmacology
  • Leishmania / drug effects
  • Pentamidine / chemistry
  • Structure-Activity Relationship

Substances

  • Antiprotozoal Agents
  • Hydrazones
  • Pentamidine