Literature DB >> 22985960

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

Rachel L Clark1, Carol J Clements, Michael P Barrett, Simon P Mackay, Rajendra P Rathnam, George Owusu-Dapaah, John Spencer, Judith K Huggan.   

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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22985960     DOI： 10.1016/j.bmc.2012.08.049

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  2 in total

1.  Discovery of Quinazoline-2,4(1H,3H)-Dione Derivatives as Potential Antibacterial Agent: Design, Synthesis, and Their Antibacterial Activity.

Authors:  Nader M Boshta; Farag A El-Essawy; Mohammed B Alshammari; Safaa G Noreldein; Osama M Darwesh
Journal:  Molecules       Date:  2022-06-15       Impact factor: 4.927

2.  Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.

Authors:  Irene Sola; Albert Artigas; Martin C Taylor; F Javier Pérez-Areales; Elisabet Viayna; M Victòria Clos; Belén Pérez; Colin W Wright; John M Kelly; Diego Muñoz-Torrero
Journal:  Bioorg Med Chem       Date:  2016-08-22       Impact factor: 3.641
  2 in total

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