新型革兰氏阴性抗毒力药物的发现：新型大肠杆菌WaaC抑制剂的结构与性质
Discovery of new Gram-negative antivirulence drugs: structure and properties of novel E. coli WaaC inhibitors.
作者信息
Moreau F, Desroy N, Genevard J M, Vongsouthi V, Gerusz V, Le Fralliec G, Oliveira C, Floquet S, Denis A, Escaich S, Wolf K, Busemann M, Aschenbrenner A
机构信息
MUTABILIS SA, 102 Avenue Gaston Roussel, 93230 Romainville, France.
出版信息
Bioorg Med Chem Lett. 2008 Jul 15;18(14):4022-6. doi: 10.1016/j.bmcl.2008.05.117. Epub 2008 Jun 5.
Heptosyltransferases such as WaaC represent promising and attractive targets for the discovery of new Gram-negative antibacterial drugs based on antivirulence mechanisms. We report herein our approach to the identification of the first micromolar inhibitors of WaaC and the preliminary SAR generated from this family of 2-aryl-5-methyl-4-(5-aryl-furan-2-yl-methylene)-2,4-dihydro-pyrazol-3-ones identified by virtual screening.
像WaaC这样的庚糖基转移酶是基于抗毒力机制发现新型革兰氏阴性抗菌药物的有前景且具吸引力的靶点。我们在此报告我们鉴定WaaC的首个微摩尔级抑制剂的方法，以及由通过虚拟筛选鉴定出的这一系列2-芳基-5-甲基-4-(5-芳基-呋喃-2-基亚甲基)-2,4-二氢-吡唑-3-酮产生的初步构效关系。
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