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The Strathprints institutional repository is a digital archive of University of Strathclyde's Open Access research outputs. Strathprints provides access to thousands of Open Access research papers by Strathclyde researchers, including by researchers from the Physical Activity for Health Group based within the School of Psychological Sciences & Health. Research here seeks to better understand how and why physical activity improves health, gain a better understanding of the amount, intensity, and type of physical activity needed for health benefits, and evaluate the effect of interventions to promote physical activity.

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

Clark, Rachel L. and Clements, Carol J. and Barrett, Michael P. and Mackay, Simon P. and Rathnam, Rajendra P. and Owusu-Dapaah, George and Spencer, John and Huggan, Judith K. (2012) Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT. Bioorganic and Medicinal Chemistry, 20 (20). pp. 6019-6033. ISSN 0968-0896

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Abstract

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.