Novel nikkomycin analogues: inhibitors of the fungal cell wall biosynthesis enzyme chitin synthase

K Obi; J Uda; K Iwase; O Sugimoto; H Ebisu; A Matsuda

doi:10.1016/s0960-894x(00)00256-0

Novel nikkomycin analogues: inhibitors of the fungal cell wall biosynthesis enzyme chitin synthase

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1451-4. doi: 10.1016/s0960-894x(00)00256-0.

Authors

K Obi¹, J Uda, K Iwase, O Sugimoto, H Ebisu, A Matsuda

Affiliation

¹ Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd, Tochigi-ken, Japan.

PMID: 10888330
DOI: 10.1016/s0960-894x(00)00256-0

Abstract

A series of novel nikkomycin analogue inhibitors of the chitin synthase of fungal cell wall was synthesized and evaluated for their inhibitory activities. Among them, the compound having a phenanthrene group at the terminal amino acid was found to possess strong anti-chitin synthase activity.

MeSH terms

Amino Acid Substitution
Aminoglycosides*
Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / metabolism
Anti-Bacterial Agents / pharmacology*
Binding Sites
Candida / enzymology
Cell Wall / enzymology
Chitin Synthase / antagonists & inhibitors*
Drug Design
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / metabolism
Enzyme Inhibitors / pharmacology
Molecular Structure
Protein Conformation

Substances

Aminoglycosides
Anti-Bacterial Agents
Enzyme Inhibitors
nikkomycin
Chitin Synthase