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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.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Clark RL,Clements CJ,Barrett MP,Mackay SP,Rathnam RP,Owusu-Dapaah G,Spencer J,Huggan JK

doi

10.1016/j.bmc.2012.08.049

subject

Has Abstract

pub_date

2012-10-15 00:00:00

pages

6019-33

issue

20

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00671-2

journal_volume

20

pub_type

杂志文章

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