1416772-63-8Relevant articles and documents
Synthesis and antimycobacterial activity of 2,1′-dihydropyridomycins
Horlacher, Oliver P.,Hartkoorn, Ruben C.,Cole, Stewart T.,Altmann, Karl-Heinz
, p. 264 - 268 (2013/03/29)
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.