Synthesis of 2-(pyrimidin-2-yl)-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carbolines as antileishmanial agents

  • Eur J Med Chem. 2010 Aug;45(8):3274-80. doi: 10.1016/j.ejmech.2010.04.004.
Ravi Kumar  1 ,  Shahnawaz Khan ,  Aditya Verma ,  Saumya Srivastava ,  Preeti Viswakarma ,  Suman Gupta ,  Sanjeev Meena ,  Neetu Singh ,  Jayanta Sarkar ,  Prem M S Chauhan
Affiliations
  • 1. Medicinal & Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India.
PMID: 20457476 DOI: 10.1016/j.ejmech.2010.04.004
Abstract

A series of 2-(pyrimidin-2-yl)-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline derivatives has been synthesized and evaluated for antileishmanial activity against Leishmania donovani. Compound 8 exhibited best antileishmanial activity with IC(50) value of 1.93 microg/ml against amastigotes, high selectivity index, and was more active than reference drugs sodium stilbogluconate and pentamidine.