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World class computing and information science research at Strathclyde...

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 University of Strathclyde researchers, including by researchers from the Department of Computer & Information Sciences involved in mathematically structured programming, similarity and metric search, computer security, software systems, combinatronics and digital health.

The Department also includes the iSchool Research Group, which performs leading research into socio-technical phenomena and topics such as information retrieval and information seeking behaviour.

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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.