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

被引:55
作者
Thirkettle, J
Alvarez, E
Boyd, H
Brown, M
Diez, E
Hueso, J
Elson, S
Fulston, M
Gershater, C
Morata, ML
Perez, P
Ready, S
Sanchez-Puelles, JM
Sheridan, R
Stefanska, A
Warr, S
机构
[1] SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
[2] SmithKline Beecham Pharmaceut SA, Ctr Invest Basica, Madrid 28760, Spain
[3] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England
关键词
D O I
10.7164/antibiotics.53.664
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Two new classes of inhibitors of LpPLA(2) 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 patent and selective competitive inhibitors of LpPLA(2).
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页码:664 / 669
页数:6
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