Synthesis and evaluation of novel pyrrolidinyl sordaricin derivatives as antifungal agents

Masami Arai; Tamako Harasaki; Takashi Fukuoka; Satoru Kaneko; Toshiyuki Konosu

doi:10.1016/s0960-894x(02)00534-6

Synthesis and evaluation of novel pyrrolidinyl sordaricin derivatives as antifungal agents

Bioorg Med Chem Lett. 2002 Oct 7;12(19):2733-6. doi: 10.1016/s0960-894x(02)00534-6.

Authors

Masami Arai¹, Tamako Harasaki, Takashi Fukuoka, Satoru Kaneko, Toshiyuki Konosu

Affiliation

¹ Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., 2-58, Hiromachi 1-chome, Shinagawa-ku, Tokyo, Japan.

PMID: 12217365
DOI: 10.1016/s0960-894x(02)00534-6

Abstract

N-Benzyl pyrrolidinyl sordaricin derivatives have been synthesized from cis-4-hydroxy-D-proline in a stereocontrolled manner. These compounds maintained moderate antifungal activity against several pathogenic fungal strains. Their MIC values against Candida albicans were in the range of 0.25-2 microg/mL.

MeSH terms

Antifungal Agents / chemical synthesis*
Antifungal Agents / pharmacology*
Diterpenes
Fluconazole / pharmacology
Fungi / drug effects
Indicators and Reagents
Microbial Sensitivity Tests
Pyrrolidinones / chemical synthesis*
Pyrrolidinones / pharmacology*

Substances

Antifungal Agents
Diterpenes
Indicators and Reagents
Pyrrolidinones
sordaricin
Fluconazole