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

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

Research output: Contribution to journalArticle

16 Citations (Scopus)

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 mu M. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. (C) 2012 Elsevier Ltd. All rights reserved.

LanguageEnglish
Pages6019-6033
Number of pages15
JournalBioorganic and Medicinal Chemistry
Volume20
Issue number20
DOIs
Publication statusPublished - 15 Oct 2012

Fingerprint

Quinazolines
African Trypanosomiasis
Trypanosoma brucei brucei
Scaffolds
Libraries
Parasites
Derivatives
Bz-423

Keywords

  • identification
  • development
  • 1,4-benzodiazepin-2-one
  • quinazoline-2,4-dione scaffolds
  • submicromolar inhibitors
  • HAT
  • trypanosomiasis
  • benzodiazepines

Cite this

Clark, Rachel L. ; Clements, Carol J. ; Barrett, Michael P. ; Mackay, Simon P. ; Rathnam, Rajendra P. ; Owusu-Dapaah, George ; Spencer, John ; Huggan, Judith K. / Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT. In: Bioorganic and Medicinal Chemistry. 2012 ; Vol. 20, No. 20. pp. 6019-6033.
@article{916edc53ccc04a3780748e7a58a0632a,
title = "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 mu M. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. (C) 2012 Elsevier Ltd. All rights reserved.",
keywords = "identification , development , 1,4-benzodiazepin-2-one , quinazoline-2,4-dione scaffolds , submicromolar inhibitors , HAT , trypanosomiasis, benzodiazepines",
author = "Clark, {Rachel L.} and Clements, {Carol J.} and Barrett, {Michael P.} and Mackay, {Simon P.} and Rathnam, {Rajendra P.} and George Owusu-Dapaah and John Spencer and Huggan, {Judith K.}",
year = "2012",
month = "10",
day = "15",
doi = "10.1016/j.bmc.2012.08.049",
language = "English",
volume = "20",
pages = "6019--6033",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
number = "20",

}

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; Huggan, Judith K.

In: Bioorganic and Medicinal Chemistry, Vol. 20, No. 20, 15.10.2012, p. 6019-6033.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT

AU - Clark, Rachel L.

AU - Clements, Carol J.

AU - Barrett, Michael P.

AU - Mackay, Simon P.

AU - Rathnam, Rajendra P.

AU - Owusu-Dapaah, George

AU - Spencer, John

AU - Huggan, Judith K.

PY - 2012/10/15

Y1 - 2012/10/15

N2 - 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 mu M. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. (C) 2012 Elsevier Ltd. All rights reserved.

AB - 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 mu M. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds. (C) 2012 Elsevier Ltd. All rights reserved.

KW - identification

KW - development

KW - 1,4-benzodiazepin-2-one

KW - quinazoline-2,4-dione scaffolds

KW - submicromolar inhibitors

KW - HAT

KW - trypanosomiasis

KW - benzodiazepines

UR - http://www.scopus.com/inward/record.url?scp=84866944696&partnerID=8YFLogxK

U2 - 10.1016/j.bmc.2012.08.049

DO - 10.1016/j.bmc.2012.08.049

M3 - Article

VL - 20

SP - 6019

EP - 6033

JO - Bioorganic and Medicinal Chemistry

T2 - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

IS - 20

ER -