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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

journal contribution
posted on 2023-06-08, 18:34 authored by Rachel L Clark, Carol J Clements, Michael P Barrett, Simon P Mackay, Rajendra P Rathnam, George Owusu-Dapaah, John SpencerJohn Spencer, Judith K Huggan
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.

History

Publication status

  • Published

Journal

Bioorganic and Medicinal Chemistry

ISSN

0968-0896

Publisher

Elsevier

Issue

20

Volume

20

Page range

6019-6033

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2014-09-30

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