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Identification of a broad-spectrum azasordarin with improved pharmacokinetic properties.

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.

Date de publication
17 April 2003
Chercheur(euse)s
Serrano-Wu MH, Laurent DR, Carroll TM, Dodier M, Gao Q, Gill P, Quesnelle C, Marinier A, Mazzucco CE, Regueiro-Ren A, Stickle TM, Wu D, Yang H, Yang Z, Zheng M, Zoeckler ME, Vyas DM, Balasubramanian BN
Référence PubMed
Bioorg. Med. Chem. Lett. 2003;13(8):1419-23
ID PubMed
12668003
Affiliation
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. michael.serrano-wu@bms.com