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; Judith K. Huggan

Journal Article

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 (2012) 20(20) 6019-6033

DOI: 10.1016/j.bmc.2012.08.049

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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 μM. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. © 2012 Elsevier Ltd. All rights reserved.

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Clark, R. L., Clements, C. J., Barrett, M. P., MacKay, S. P., Rathnam, R. P., Owusu-Dapaah, G., … Huggan, J. 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), 6019–6033. https://doi.org/10.1016/j.bmc.2012.08.049

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

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