Syntheses of new substituted triazino tetrahydroisoquinolines and beta-carbolines as novel antileishmanial agents

Eur J Med Chem. 2006 Jan;41(1):106-13. doi: 10.1016/j.ejmech.2005.09.007. Epub 2005 Dec 13.

Abstract

A series of triazino tetrahydroisoquinolines (3-5) and beta-carboline derivatives (15-27) have been synthesized as novel antileishmanial agents. Among them, compounds 15, 16 and 25 have shown 78.0%, 78.6% and 68.0% in vivo inhibition against Leishmania donovani at a dose of 50 mg kg(-1) x 5 days, respectively, while compounds 3 and 18 exhibited 55.6% and 53.3% in vivo inhibitions, respectively, against L. donovani at a dose of 50 mg kg(-1) x 5 days.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology
  • Carbolines / chemical synthesis*
  • Carbolines / chemistry
  • Carbolines / pharmacology
  • Cricetinae
  • Inhibitory Concentration 50
  • Leishmania donovani / drug effects*
  • Mesocricetus
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Structure-Activity Relationship
  • Tetrahydroisoquinolines / chemical synthesis*
  • Tetrahydroisoquinolines / chemistry
  • Tetrahydroisoquinolines / pharmacology
  • Triazines / chemistry*

Substances

  • Antiprotozoal Agents
  • Carbolines
  • Tetrahydroisoquinolines
  • Triazines