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Identification of a broad-spectrum azasordarin with improved pharmacokinetic properties
Michael H Serrano-Wu1, Denis R St Laurent, Tina M Carroll
1Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. michael.serrano-wu@bms.com
Bioorganic & Medicinal Chemistry Letters
|April 2, 2003
Abstract:
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.