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

Ravi Kumar; Shahnawaz Khan; Aditya Verma; Saumya Srivastava; Preeti Viswakarma; Suman Gupta; Sanjeev Meena; Neetu Singh; Jayanta Sarkar; Prem M S Chauhan

doi:10.1016/j.ejmech.2010.04.004

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. Epub 2010 Apr 14.

Authors

Ravi Kumar¹, Shahnawaz Khan, Aditya Verma, Saumya Srivastava, Preeti Viswakarma, Suman Gupta, Sanjeev Meena, Neetu Singh, Jayanta Sarkar, Prem M S Chauhan

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antiprotozoal Agents / chemical synthesis*
Antiprotozoal Agents / chemistry
Antiprotozoal Agents / pharmacology*
Antiprotozoal Agents / toxicity
Carbolines / chemical synthesis*
Carbolines / chemistry
Carbolines / pharmacology*
Carbolines / toxicity
Cell Line
Cell Survival / drug effects
Inhibitory Concentration 50
Leishmania donovani / drug effects*
Mice

Substances

Antiprotozoal Agents
Carbolines