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

Clark, Rachel L, Clements, Carol J, Barrett, Michael P, Mackay, Simon P, Rathnam, Rajendra P, Owusu-Dapaah, George, 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 & 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 μM. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science
Depositing User: Deeptima Massey
Date Deposited: 30 Sep 2014 11:21
Last Modified: 30 Sep 2014 11:21
URI: http://sro.sussex.ac.uk/id/eprint/50424
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