Sign in
Back
Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT
Journal article   Peer reviewed

Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT

Rachel L. Clark, Carol J. Clements, Michael P. Barrett, Simon P. Mackay, Rajendra P. Rathnam, George Owusu-Dapaah, John Spencer and Judith K. Huggan
Bioorganic & medicinal chemistry, Vol.20(20), pp.6019-6033
15/10/2012
DOI: https://doi.org/10.1016/j.bmc.2012.08.049
PMID: 22985960

Abstract

Biochemistry & Molecular Biology Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology
A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 mu M. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. (C) 2012 Elsevier Ltd. All rights reserved.

Metrics

1 Record Views

Details