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1.发明公开8/17 HETEROCYCLIC COMPOUNDS AND USES THEREOF AS D-ALANYL-D-ALANINE LIGASE INHIBITORS 审中-公开8/17杂环化合物和它们作为D-丙氨酰-D-丙氨酸连接酶抑制剂
公开(公告)号：EP1411949A4
公开(公告)日：2004-11-24
申请号：EP02759101
申请日：2002-06-28
发明人： MOE SCOTT T , ALA PAUL J , PEROLA EMANUELE , FAERMAN CARLOS H , CLEMENT JACOB J , ALI JANID A , WILL PAUL M , MARCHESE SALVATORE A , MAGEE ANDREW S , GAZZANIGA JOHN V , FARADY CHRISTOPHER , NAVIA MANUEL A , CONNELLY PATRICK R
IPC分类号： A61K31/519 , A61K31/525 , A61P31/04 , C07D401/12 , C07D471/04 , C07D475/08 , C07D487/02 , C07D487/04 , C07D519/00 , A61K31/517
CPC分类号： C07D401/12 , C07D471/04 , C07D475/08 , C07D487/04
摘要： The invention is based on the discovery of a new class of heterocyclic compounds having, for example, antibacterial properties. The D-Ala-D-Ala ligase enzyme is a critical pathway enzyme in the bacterial cell-wall synthesis. The compounds can bind to and inhibit the enzyme D-Ala-D-Ala ligase. The new compounds' activity combined with their ability to cross bacterial cell membranes makes them suitable for use as antibacterial drugs or other antibacterial applications.
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2.发明公开STRUCTURE-BASED DRUG DESIGN METHODS FOR IDENTIFYING D-ALA-D-ALA LIGASE INHIBITORS AS ANTIBACTERIAL DRUGS 审中-公开主动设计工艺对结构基础一种判别D-ALA-D-ALA-连接酶抑制剂AS抗菌物质
公开(公告)号：EP1412516A4
公开(公告)日：2004-09-08
申请号：EP02749688
申请日：2002-06-28
发明人： NAVIA MANUEL A , ALA PAUL J , GRIFFITH JAMES P , ALI JANID A , FAERMAN CARLOS H , MOE SCOTT T , MAGEE ANDREW S , CONNELLY PATRICK R , PEROLA EMANUELE
CPC分类号： C12N9/93
摘要： The invention is based on the discovery that certain small molecules can bind to the ATP binding site of D-Ala-D-Ala ligase, even in the absence of the enzyme's substrate, and can cause a conformational change in the enzyme structure similar to that which occurs upon binding of ATP and substrate to the enzyme. Without wishing to be bound by any theory, it is believed that such a conformational change is required for either activation or inhibition of the enzyme. The information obtained from this discovery has enabled identification of key interactions in the active site of the enzyme, as well as the design and opimization of inhibitors.
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