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Studies on n-octyl-5-(alpha-D-arabinofuranosyl)-beta-D-galactofuranosides for mycobacterial glycosyltransferase activity

Lookup NU author(s): Dr Sudagar Gurcha, Professor Del Besra

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Abstract

The mycobacterial cell wall is a potential target for new drug development. Herein we report the preparation and activity of several n-octyl-5-(alpha-D-arabinofuranosyl)-beta-D-galactofuranoside derivatives. A cell-free assay system has been utilized for determination of the ability of disaccharide analogues to act as arabinosyltransferase acceptors using [C-14]-DPA as the glycosyl donor. In addition, in vitro inhibitory activity has been determined in a colorimetric broth microdilution assay system against MTB H37Ra and three clinical isolates of Mycobacterium avium complex (MAC). One of these disaccharides showed moderate activity against MTB. The biological evaluation of these disaccharides suggests that more hydrophobic analogues with a blocked reducing end showed better activity as compared to a totally deprotected disaccharide that more closely resembles the natural substrates in cell wall biosynthesis. (C) 2002 Elsevier Science Ltd. All rights reserved.


Publication metadata

Author(s): Pathak AK, Pathak V, Suling WJ, Gurcha SS, Morehouse CB, Besra GS, Maddry JA, Reynolds RC

Publication type: Article

Publication status: Published

Journal: Bioorganic & Medicinal Chemistry

Year: 2002

Volume: 10

Issue: 4

Pages: 923-928

ISSN (print): 0968-0896

ISSN (electronic): 1464-3391

Publisher: Pergamon

URL: http://dx.doi.org/10.1016/S0968-0896(01)00343-1

DOI: 10.1016/S0968-0896(01)00343-1


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Funding

Funder referenceFunder name
CA-13148NCI NIH HHS
R01 AI045317NIAID NIH HHS
N01 AI095364NIAID NIH HHS
R01AI45317NIAID NIH HHS

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