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首页> 外文期刊>The Journal of Antibiotics: An International Journal >A new series of the SMTP plasminogen modulators with a phenylamine-based side chain
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A new series of the SMTP plasminogen modulators with a phenylamine-based side chain

机译：具有苯胺基侧链的新系列SMTP纤溶酶原调节剂

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摘要

SMTPs are a family of small-molecule plasminogen modulators that enhance plasminogen activation. SMTP-7, one of the most potent congeners, is effective in treating thrombotic cerebral infarction. The SMTP molecule consists of a tricyclic gamma;-lactam moiety, a geranylmethyl group, and an N-linked side chain. The presence of both an aromatic group and a negatively ionizable group in the N-linked side chain is crucial for activity. Investigations of the congeners with a phenylglycine-based side chain suggest that a phenolic hydroxy group affects potency. In this study, we isolate and characterize a series of novel SMTP congeners with a phenylamine-based N-linked side chain. Of the 11 congeners isolated, SMTP-19 (with a 4-phenylcarboxylic acid moiety), SMTP-22 (with a 3-hydroxyphenyl-4-carboxylic acid moiety) and SMTP-25 (with a 2-hydroxyphenyl-3-carboxylic acid moiety) are as potent as SMTP-7 in plasminogen-modulating activity. Their isomers with a carboxylic acid group and/or a phenolic hydroxy group at different positions have 40% of the activity of these congeners. Both SMTP-22 and SMTP-25 have 1.7 times more oxygen radical absorbance capacity as compared with SMTP-7.
机译：SMTP是增强纤溶酶原激活的小分子纤溶酶原调节剂家族。 SMTP-7是最有效的同类药物之一，可有效治疗血栓性脑梗塞。 SMTP分子由三环γ-内酰胺部分，香叶基甲基和N-连接的侧链组成。 N-连接侧链中同时存在芳族基团和可负电离的基团对于活性至关重要。对具有基于苯基甘氨酸的侧链的同类物的研究表明，酚羟基会影响效能。在这项研究中，我们分离并表征了一系列具有苯胺基N-连接侧链的新型SMTP同系物。在分离的11个同类物中，SMTP-19（具有4-苯基羧酸部分），SMTP-22（具有3-羟基苯基-4-羧酸部分）和SMTP-25（具有2-羟基苯基-3-羧酸部分）部分）的纤溶酶原调节活性与SMTP-7一样强。它们在不同位置具有羧酸基和/或酚羟基的异构体具有这些同类物活性的＜40％。与SMTP-7相比，SMTP-22和SMTP-25的氧自由基吸收能力均高1.7倍以上。

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