Synthesis and Antimycobacterial Activity of 2,1鈥?Dihydropyridomycins
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- 作者：Oliver P. Horlacher ; Ruben C. Hartkoorn ; Stewart T. Cole ; Karl-Heinz Altmann
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：February 14, 2013
- 年：2013
- 卷：4
- 期：2
- 页码：264-268
- 全文大小：267K
- 年卷期：v.4,no.2(February 14, 2013)
- ISSN：1948-5875
文摘
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.