Novel antifungal beta-amino acids: synthesis and activity against Candida albicans

Joachim Mittendorf; Franz Kunisch; Michael Matzke; Hans-Christian Militzer; Axel Schmidt; Wolfgang Schönfeld

doi:10.1016/s0960-894x(02)00958-7

Novel antifungal beta-amino acids: synthesis and activity against Candida albicans

Bioorg Med Chem Lett. 2003 Feb 10;13(3):433-6. doi: 10.1016/s0960-894x(02)00958-7.

Authors

Joachim Mittendorf¹, Franz Kunisch, Michael Matzke, Hans-Christian Militzer, Axel Schmidt, Wolfgang Schönfeld

Affiliation

¹ Medicinal Chemistry, Business Group Pharma, Bayer AG, D-42096 Wuppertal, Germany. joachim.mittendorf.jm@bayer-ag.de

PMID: 12565945
DOI: 10.1016/s0960-894x(02)00958-7

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.

MeSH terms

Amino Acids / chemical synthesis*
Amino Acids / pharmacology*
Antifungal Agents / chemical synthesis*
Antifungal Agents / pharmacology*
Candida albicans / drug effects*
Indicators and Reagents
Microbial Sensitivity Tests
Molecular Conformation
Stereoisomerism
Structure-Activity Relationship

Substances

Amino Acids
Antifungal Agents
Indicators and Reagents