EPSP SYNTHASE INHIBITOR DESIGN .3. SYNTHESIS AND EVALUATION OF A NEW 5-OXAMIC ACID ANALOG OF EPSP WHICH INCORPORATES A MALONATE ETHER AS A 3-PHOSPHATE MIMIC

被引：5

作者：

COREY, SD

PANSEGRAU, PD

WALKER, MC

SIKORSKI, JA

机构：

[1] MONSANTO CO,MONSANTO CORP RES,700 CHESTERFIELD PKWY N,ST LOUIS,MO 63198

[2] MONSANTO CO,DIV NEW PROD,AGR CORP,ST LOUIS,MO 63198

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80779-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The unusual shikimate oxamic acid analog 3, containing a 3-malonate ether, was synthesized and found to be a potent product-analog inhibitor of EPSP synthase (K(i) = 5.2 +/- 0.2 muM). The potency of 3 confirms that these 3-malonate ethers function as effective 3-phosphate replacements in this system and that the oxamic acid moiety represents an unusual mimetic of the EPSP carboxyvinyl ether group.

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页码：2857 / 2862

页数：6

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