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Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity
Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity
A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 µM.
0968-0896
1802-1815
Spencer, John
a3cf55cd-a4c7-4af6-b16c-96c8fb8c4cf4
Rathnam, Rajendra P.
2c3d1196-015c-4dc0-8385-a46cf6a28545
Harvey, Alan L.
af2bc8ce-8c4b-4724-a610-8d2512bc18a8
Clements, Carol J.
2c25a25f-2ca4-4e3b-8e6e-97ee17f0c933
Clark, Rachel L.
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Barrett, Michael P.
e2e4193c-e1eb-424d-9974-4f1258d1d0ae
Wong, Pui Ee
7ca1d927-6f47-4720-aa91-4738973f5531
Male, Louise
89b88c4f-2308-4b94-8f3a-2dc537a66533
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Mackay, Simon P.
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Spencer, John
a3cf55cd-a4c7-4af6-b16c-96c8fb8c4cf4
Rathnam, Rajendra P.
2c3d1196-015c-4dc0-8385-a46cf6a28545
Harvey, Alan L.
af2bc8ce-8c4b-4724-a610-8d2512bc18a8
Clements, Carol J.
2c25a25f-2ca4-4e3b-8e6e-97ee17f0c933
Clark, Rachel L.
905c3c5d-1921-4667-82a0-4b7375503d1f
Barrett, Michael P.
e2e4193c-e1eb-424d-9974-4f1258d1d0ae
Wong, Pui Ee
7ca1d927-6f47-4720-aa91-4738973f5531
Male, Louise
89b88c4f-2308-4b94-8f3a-2dc537a66533
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Mackay, Simon P.
623f9830-c609-4b43-a30a-96f5c614d08f

Spencer, John, Rathnam, Rajendra P., Harvey, Alan L., Clements, Carol J., Clark, Rachel L., Barrett, Michael P., Wong, Pui Ee, Male, Louise, Coles, Simon J. and Mackay, Simon P. (2011) Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. Bioorganic & Medicinal Chemistry, 19 (5), 1802-1815. (doi:10.1016/j.bmc.2011.01.010).

Record type: Article

Abstract

A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 µM.

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More information

Published date: 1 March 2011
Related URLs:
Organisations: Organic Chemistry: Synthesis, Catalysis and Flow

Identifiers

Local EPrints ID: 346144
URI: http://eprints.soton.ac.uk/id/eprint/346144
DOI: doi:10.1016/j.bmc.2011.01.010
ISSN: 0968-0896
PURE UUID: d7ad308b-e03e-4a0f-9926-2b8730cbec3d
ORCID for Simon J. Coles: ORCID iD orcid.org/0000-0001-8414-9272

Catalogue record

Date deposited: 20 Dec 2012 13:49
Last modified: 15 Mar 2024 03:01

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Contributors

Author: John Spencer
Author: Rajendra P. Rathnam
Author: Alan L. Harvey
Author: Carol J. Clements
Author: Rachel L. Clark
Author: Michael P. Barrett
Author: Pui Ee Wong
Author: Louise Male
Author: Simon J. Coles ORCID iD
Author: Simon P. Mackay

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