Publication

Synthesis and Antimycobacterial Activity of 2,1 '-Dihydropyridomycins

Stewart Cole, Ruben Hartkoorn
2013
Journal Articles

Abstract

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.

Official source

https://infoscience.epfl.ch/entities/publication/02e106d5-baca-455b-9a77-b88b4952b463

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