1416772-64-9Relevant academic research and scientific papers
PYRIDOMYCIN BASED COMPOUNDS EXHIBITING AN ANTITUBERCULAR ACTIVITY
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Paragraph 0173-0180, (2015/10/05)
Formula (1), X1 represents O or NR6, X2 represents O or NR6, X3 represents O or NR1, R1 represents H or C1 to C3 alkyl, R2 represents H, or linear or branched C1-C8 alkyl optionally including one or more heteroatoms, cyclopropyl, cyclobutyl, cyclohexyl or oxetanyl or amino acid side chain or protected amino acid side chain, or R1 and R2 may form together a saturated, partly saturated or unsaturated 5 or 6 membered ring system, optionally substituted, R3 represents H, cyclopentyl, cyclohexyl, aryl or hydroxyaryl, aryl or hydroxyaryl being optionally substituted by fluorine, or linear or branched C1 to C8 alkyl optionally including a hetero atom, R4 represents phenyl or 5- or 6-membered heterocycles including one or more nitrogen or oxygen atoms optionally substituted with 1 to 4, respectively 5 fluorine atoms, and R6 represents H, or linear or branched alkyl chain having 1 to 3 carbon atoms.
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.
