TY - JOUR
T1 - The Abyssomicin C family as in vitro inhibitors of Mycobacterium tuberculosis
AU - Freundlich, Joel S.
AU - Lalgondar, Mallikarjun
AU - Wei, Jun Rong
AU - Swanson, Stephanie
AU - Sorensen, Erik J.
AU - Rubin, Eric J.
AU - Sacchettini, James C.
N1 - Funding Information:
This work was supported by the Bill and Melinda Gates Foundation (grant 42844 ). J.C.S. acknowledges the Robert A. Welch Foundation (grant A-0015 ).
Copyright:
Copyright 2012 Elsevier B.V., All rights reserved.
PY - 2010/9
Y1 - 2010/9
N2 - The antimycobacterial efficacy of the abyssomicin C family of natural products, in addition to a key synthetic intermediate, has been investigated given their reported inhibition of Bacillus subtilis p-aminobenzoate biosynthesis. The naturally occurring (-)-abyssomicin C and its atropisomer were found to exhibit low micromolar growth inhibition against the relatively fast-growing and non-virulent Mycobacterium smegmatis and the vaccine strain Mycobacterium bovis BCG, while their antipodes were slightly less active. (-)-Abyssomicin C and its atropisomer were particularly efficacious against Mycobacterium tuberculosis H37Rv, exhibiting MIC values of 3.6 and 7.2 μM, respectively. More specifically, (-)-abyssomicin C was bactericidal. This complex natural product and its analogs, thus, hold promise as chemical tools in the study of M. tuberculosis metabolism.
AB - The antimycobacterial efficacy of the abyssomicin C family of natural products, in addition to a key synthetic intermediate, has been investigated given their reported inhibition of Bacillus subtilis p-aminobenzoate biosynthesis. The naturally occurring (-)-abyssomicin C and its atropisomer were found to exhibit low micromolar growth inhibition against the relatively fast-growing and non-virulent Mycobacterium smegmatis and the vaccine strain Mycobacterium bovis BCG, while their antipodes were slightly less active. (-)-Abyssomicin C and its atropisomer were particularly efficacious against Mycobacterium tuberculosis H37Rv, exhibiting MIC values of 3.6 and 7.2 μM, respectively. More specifically, (-)-abyssomicin C was bactericidal. This complex natural product and its analogs, thus, hold promise as chemical tools in the study of M. tuberculosis metabolism.
KW - Abyssomicin
KW - Mycobacterium tuberculosis
KW - p-Aminobenzoate metabolism
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U2 - 10.1016/j.tube.2010.08.002
DO - 10.1016/j.tube.2010.08.002
M3 - Article
C2 - 20739223
AN - SCOPUS:77957197443
VL - 90
SP - 298
EP - 300
JO - Bulletin of the International Union Against Tuberculosis and Lung Disease
JF - Bulletin of the International Union Against Tuberculosis and Lung Disease
SN - 1472-9792
IS - 5
ER -