title: Novel antifungal beta-amino acids: synthesis and activity against Candida albicans.
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.
authors.affiliation: Medicinal Chemistry, Business Group Pharma, Bayer AG, D-42096 Wuppertal, Germany. joachim.mittendorf.jm@bayer-ag.de
authors.forename: Joachim
authors.initials: J
authors.lastname: Mittendorf
authors.forename: Franz
authors.initials: F
authors.lastname: Kunisch
authors.forename: Michael
authors.initials: M
authors.lastname: Matzke
authors.forename: Hans-Christian
authors.initials: HC
authors.lastname: Militzer
authors.forename: Axel
authors.initials: A
authors.lastname: Schmidt
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Schönfeld
mesh_terms: 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
chemical_list: D000596:Amino Acids; D000935:Antifungal Agents; D007202:Indicators and Reagents