Novel antifungal beta-amino acids: synthesis and activity against Candida albicans.
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.
Mittendorf
Joachim
J
Medicinal Chemistry, Business Group Pharma, Bayer AG, D-42096 Wuppertal, Germany. joachim.mittendorf.jm@bayer-ag.de
Kunisch
Franz
F
Matzke
Michael
M
Militzer
Hans-Christian
HC
Schmidt
Axel
A
Schönfeld
Wolfgang
W
D000596:Amino Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000596:Amino Acids; D000935:Antifungal Agents; D007202:Indicators and Reagents