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

Clark, R.L., Clements, C.J., Barrett, M.P. , Mackay, S.P., Rathnam, R.P., Owusu-Dapaah, G., Spencer, J. and 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), pp. 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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Barrett, Professor Michael
Authors: Clark, R.L., Clements, C.J., Barrett, M.P., Mackay, S.P., Rathnam, R.P., Owusu-Dapaah, G., Spencer, J., and Huggan, J.K.
College/School:College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
Journal Name:Bioorganic and Medicinal Chemistry
ISSN:0968-0896

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