依克拉普明，一种对甲氧苄啶敏感菌和耐药菌均有强效活性的新型二氨基嘧啶。
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
作者信息
Schneider Peter, Hawser Stephen, Islam Khalid
机构信息
Arpida Ltd, Dammstrasse 36, CH-4142, Muenchenstein, Switzerland.
出版信息
Bioorg Med Chem Lett. 2003 Dec 1;13(23):4217-21. doi: 10.1016/j.bmcl.2003.07.023.
Iclaprim, a new selective dihydrofolate inhibitor was synthesized based on rational drug design. Iclaprim's interaction with a resistant Staphylococcus aureus dihydrofolate reductase (DHFR) is outlined in comparison to trimethoprim (TMP). This compound is active against methicillin, TMP and vancomycin resistant strains. Arpida Ltd. is developing Iclaprim for serious hospital infections from Gram-positive pathogens and respiratory tract infections.
依克拉普明是一种基于合理药物设计合成的新型选择性二氢叶酸抑制剂。与甲氧苄啶（TMP）相比，概述了依克拉普明与耐甲氧西林金黄色葡萄球菌二氢叶酸还原酶（DHFR）的相互作用。该化合物对耐甲氧西林、耐甲氧苄啶和耐万古霉素菌株具有活性。阿皮达有限公司正在开发依克拉普明，用于治疗由革兰氏阳性病原体引起的严重医院感染和呼吸道感染。
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