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Novel antifungal beta-amino acids: synthesis and activity against Candida albicans
Joachim Mittendorf1, Franz Kunisch, Michael Matzke
1Medicinal Chemistry, Business Group Pharma, Bayer AG, D-42096 Wuppertal, Germany. joachim.mittendorf.jm@bayer-ag.de
Bioorganic & Medicinal Chemistry Letters
|February 5, 2003
Abstract:
A series of novel beta-amino acids has been synthesized and tested for their in vitro antifungal activity against Candida albicans. A steep SAR was observed. beta-Amino acid 21 (BAY 10-8888/PLD-118) revealed the most favourable activity-tolerability profile and was selected for clinical studies as a novel antifungal for the oral treatment of yeast infections.