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

Spencer, J., Rathnam, R.P., Harvey, A.L., Clements, C.J., Clark, R.L., Barrett, M.P. , Wong, P.E., Male, L., Coles, S.J. and Mackay, S.P. (2011) Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. Bioorganic and Medicinal Chemistry, 19(5), pp. 1802-1815. (doi:10.1016/j.bmc.2011.01.010)

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Publisher's URL: http://dx.doi.org/10.1016/j.bmc.2011.01.010

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 mu M.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Barrett, Professor Michael
Authors: Spencer, J., Rathnam, R.P., Harvey, A.L., Clements, C.J., Clark, R.L., Barrett, M.P., Wong, P.E., Male, L., Coles, S.J., and Mackay, S.P.
College/School:College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
Journal Name:Bioorganic and Medicinal Chemistry
Journal Abbr.:Bioorganic Med. Chem.
ISSN:0968-0896
Published Online:14 January 2011

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