Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

John Spencer; Rajendra P Rathnam; Alan L Harvey; Carol J Clements; Rachel L Clark; Michael P Barrett; Pui Ee Wong; Louise Male; Simon J Coles; Simon P Mackay

doi:10.1016/j.bmc.2011.01.010

Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

Bioorg Med Chem. 2011 Mar 1;19(5):1802-15. doi: 10.1016/j.bmc.2011.01.010. Epub 2011 Jan 14.

Authors

John Spencer¹, Rajendra P Rathnam, Alan L Harvey, Carol J Clements, Rachel L Clark, Michael P Barrett, Pui Ee Wong, Louise Male, Simon J Coles, Simon P Mackay

Affiliation

¹ School of Science, University of Greenwich at Medway, Chatham, UK. j.spencer@gre.ac.uk

PMID: 21306904
DOI: 10.1016/j.bmc.2011.01.010

Abstract

A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 μM.

Publication types

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

MeSH terms

Benzodiazepines / pharmacology*
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Microbial Sensitivity Tests
Molecular Structure
Trypanocidal Agents / chemical synthesis*
Trypanocidal Agents / chemistry
Trypanocidal Agents / pharmacology
Trypanosoma brucei brucei / drug effects*

Substances

Trypanocidal Agents
Benzodiazepines