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PAF inhibitory activity of diketopiperazines: structure-activity relationships.

作者信息

Shimazaki N, Shima I, Okamoto M, Yoshida K, Hemmi K, Hashimoto M

机构信息

Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.

出版信息

Lipids. 1991 Dec;26(12):1175-8. doi: 10.1007/BF02536526.

DOI:10.1007/BF02536526
PMID:1819704
Abstract

FR900452, a natural product isolated from the culture broth of Streptomyces phaeofaciens No. 7739, was found to inhibit PAF-induced rabbit platelet aggregation with an IC50 of 3.7 x 10(-7)M. FR900452, 1-methyl-3-[1-[5- methylthiomethyl-6-oxo-3-(2-oxo-3-cyclopenten-1-yli- dene)-2-piperazinyl]ethyl]-2-indoline, has an oxocylopentylidene group incorporated as a vinylogous amide in a diketopiperazine skeleton. This unique structure led us to synthesize diketopiperazine derivatives, 3-arylalkyl- 6-substituted-piperazine-2,5-diones. Their observed PAF inhibitory activity suggest that the D-D configuration of diketopiperazine is an important factor for anti-PAF activity and that the hydrophobic aromatic portion may play a specific role in the binding of the diketopiperazine to the PAF receptor.

摘要

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本文引用的文献

1
Studies of platelet activating factor (PAF) antagonists from microbial products. III. Pharmacological studies of FR-900452 in animal models.微生物产物中血小板活化因子（PAF）拮抗剂的研究。III. FR-900452在动物模型中的药理学研究。
Chem Pharm Bull (Tokyo). 1986 Jul;34(7):3005-10. doi: 10.1248/cpb.34.3005.
2
Diketopiperazines as a new class of platelet-activating factor inhibitors.二酮哌嗪作为一类新型血小板活化因子抑制剂。
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Diketopiperazine derivatives, a new series of platelet-activating factor inhibitors.
原核生物 tRNA 衍生环二肽生物合成的全局分析。
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Rational and combinatorial tailoring of bioactive cyclic dipeptides.生物活性环二肽的合理与组合定制
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Platelet-activating factor antagonists.血小板活化因子拮抗剂
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Studies of platelet activating factor (PAF) antagonists from microbial products. II. Pharmacological studies of FR-49175 in animal models.微生物产物来源的血小板活化因子（PAF）拮抗剂的研究。II. FR-49175在动物模型中的药理学研究。
Chem Pharm Bull (Tokyo). 1986 Jan;34(1):345-8. doi: 10.1248/cpb.34.345.
6
Studies of platelet activating factor (PAF) antagonists from microbial products. I. Bisdethiobis(methylthio)gliotoxin and its derivatives.微生物产物中血小板活化因子（PAF）拮抗剂的研究。I. 双去硫双（甲硫基）胶毒素及其衍生物。
Chem Pharm Bull (Tokyo). 1986 Jan;34(1):340-4. doi: 10.1248/cpb.34.340.