5-氨基吡唑和2-氨基噻唑的脲类化合物可抑制革兰氏阳性菌的生长。
Ureas of 5-aminopyrazole and 2-aminothiazole inhibit growth of gram-positive bacteria.
作者信息
Kane John L, Hirth Bradford H, Liang Beirong, Gourlie Brian B, Nahill Sharon, Barsomian Gary
机构信息
Genzyme Drug Discovery and Development, Genzyme Corp, Cambridge MA 02139, USA.
出版信息
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4463-6. doi: 10.1016/j.bmcl.2003.09.013.
PMID:14643347
Abstract
Ureas of 5-aminopyrazole and 2-aminothiazole emerged as lead compounds from a high-throughput screen assaying the growth of Staphylococcus aureus. Structure-activity relationships were developed for each compound series. Several compounds were also tested for activity against drug resistant strains of S. aureus in vivo.
摘要
通过高通量筛选测定金黄色葡萄球菌的生长情况，5-氨基吡唑和2-氨基噻唑的脲类化合物成为先导化合物。针对每个化合物系列建立了构效关系。还对几种化合物在体内对耐甲氧西林金黄色葡萄球菌耐药菌株的活性进行了测试。
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