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

doi:10.1016/j.bmc.2012.08.049

Paper

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

Published Oct 15, 2012 · R. Clark, C. Clements, M. Barrett

Bioorganic & medicinal chemistry

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23

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Abstract

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Study Snapshot

The most potent 1,4-benzodiazepine derivative has an MIC value of 0.97 M, making it a potential submicromolar inhibitor of Human African Trypanosomiasis.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

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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References

Risk for Human African Trypanosomiasis, Central Africa, 2000–2009

Approximately 3.5 million persons in Central Africa are at risk for human African trypanosomiasis, with five risk categories identified.

Identification of the benzodiazepines as a new class of antileishmanial agent.

Benzodiazepines show potential as a new class of antileishmanial agents, with in vitro activity comparable to sodium stibogluconate and no toxic effects on macrophages.

Trypanocidal Activity of Melamine-Based Nitroheterocycles

Melamine-based nitroheterocycles show trypanocidal activity against African trypanosomes, with no genotoxic effect in T. brucei, and no reductive or oxidative stress related to their activity.

Chemotherapy of human African trypanosomiasis: current and future prospects.

Current African trypanosomiasis treatments are unsatisfactory due to toxicity, poor efficacy, and resistance, with potential for safer and more effective drugs in the medium and long term.

Preparation and biological activity of novel tricyclic GPIIb/IIIa antagonists.

Novel tricyclic GPIIb/IIIa antagonists show potential as antithrombotic agents with increased potency compared to existing antiplatelet agents.

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