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research article
Synthesis and Antimycobacterial Activity of 2,1 '-Dihydropyridomycins
Dihydropyridomycins 2 and 3, which lack the characteristic enol ester moiety of the potent antimycobacterial natural product pyridomycin (1), have been prepared from L-Thr, R- and S-hydroxy isovaleric acid, and 3-pyridinecarboxaldehyde. The 2R isomer 2 shows only 4-fold lower anti-Mtb activity than 1, indicating that the enol ester moiety in the natural product is not critical for its biological activity. This finding establishes 2 as a potent and more practical lead for anti-TB drug discovery.
Type
research article
Web of Science ID
WOS:000315182000029
Authors
Publication date
2013
Publisher
Published in
Volume
4
Issue
2
Start page
264
End page
268
Peer reviewed
REVIEWED
EPFL units
Available on Infoscience
March 28, 2013
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