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
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作者:
Thirkettle, J
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Thirkettle, J
Alvarez, E
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Alvarez, E
Boyd, H
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Boyd, H
Brown, M
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Brown, M
Diez, E
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Diez, E
Hueso, J
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Hueso, J
Elson, S
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Elson, S
Fulston, M
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Fulston, M
Gershater, C
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Gershater, C
Morata, ML
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Morata, ML
Perez, P
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Perez, P
Ready, S
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Ready, S
Sanchez-Puelles, JM
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Sanchez-Puelles, JM
Sheridan, R
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Sheridan, R
Stefanska, A
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
Stefanska, A
Warr, S
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机构:SmithKline Beecham Pharmaceut, Worthing BN14 8QH, W Sussex, England
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
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).