Bioorganic and Medicinal Chemistry Letters p. 1419 - 1423 (2003)
Update date:2022-08-03
Topics:
Serrano-Wu, Michael H.
St. Laurent, Denis R.
Carroll, Tina M.
Dodier, Marco
Gao, Qi
Gill, Patrice
Quesnelle, Claude
Marinier, Anne
Mazzucco, Charles E.
Regueiro-Ren, Alicia
Stickle, Terry M.
Wu, Dedong
Yang, Hyekyung
Yang, Zheng
Zheng, Ming
Zoeckler, Mary E.
Vyas, Dolatrai M.
Balasubramanian, Balu N.
The synthesis and antifungal activity of 5′- and 5′-6′-substituted azasordarin derivatives are described. Modification of the 5′-position led to the discovery of the spirocyclopentyl analogue 7g, which is the first azasordarin to register single-digit MIC values versus Aspergillus spp. Further investigation identified the 5′-i-Pr derivative 7b, which displays superior pharmacokinetic properties compared to other azasordarins.
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