SB-253514 and analogues; novel inhibitors of lipoprotein-associated phospholipase A2 produced by Pseudomonas fluorescens DSM 11579. I. Fermentation of producing strain, isolation and biological activity

Two new classes of inhibitors of LpPLA2 have been identified in fermentations of Pseudomonas fluorescens. The two structurally isomeric series differ in the geometry of closure of the bicyclic carbamate and comprise a range of compounds varying only in length of their lipophilic sidechain. The most...

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Bibliographic Details
Published in:	Journal of antibiotics Vol. 53; no. 7; p. 664
Main Authors:	Thirkettle, J, Alvarez, E, Boyd, H, Brown, M, Diez, E, Hueso, J, Elson, S, Fulston, M, Gershater, C, Morata, M L, Perez, P, Ready, S, Sanchez-Puelles, J M, Sheridan, R, Stefanska, A, Warr, S
Format:	Journal Article
Language:	English
Published:	Japan 2000
Subjects:	1-Alkyl-2-acetylglycerophosphocholine Esterase Animals Bridged Bicyclo Compounds, Heterocyclic - isolation & purification Bridged Bicyclo Compounds, Heterocyclic - metabolism Bridged Bicyclo Compounds, Heterocyclic - pharmacology Drug Evaluation, Preclinical - methods Enzyme Inhibitors - isolation & purification Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Fermentation Humans Phospholipases A - antagonists & inhibitors Phospholipases A2 Pseudomonas fluorescens - metabolism Pyrans - isolation & purification Pyrans - metabolism Pyrans - pharmacology Rabbits
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Summary:	Two new classes of inhibitors of LpPLA2 have been identified in fermentations of Pseudomonas fluorescens. The two structurally isomeric series differ in the geometry of closure of the bicyclic carbamate and comprise a range of compounds varying only in length of their lipophilic sidechain. The most abundant species were extracted from the cells and purified by silica and C18 chromatography. Members of the more stable class were shown to be potent and selective competitive inhibitors of LpPLA2.
ISSN:	0021-8820
DOI:	10.7164/antibiotics.53.664