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A hypoxia-activated antibacterial prodrug.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-27 , DOI: 10.1016/j.bmcl.2020.127140 Yuan Qi Yeoh 1 , John R Horsley 1 , Steven W Polyak 2 , Andrew D Abell 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-27 , DOI: 10.1016/j.bmcl.2020.127140 Yuan Qi Yeoh 1 , John R Horsley 1 , Steven W Polyak 2 , Andrew D Abell 1
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A prodrug based on a known antibacterial compound is reported to target Staphylococcus aureus and Escherichia coli under reductive conditions. The prodrug was prepared by masking the N-terminus and side chain amines of a component lysine residue as 4-nitrobenzyl carbamates. Activation to liberate the antibacterial was demonstrated on treatment with a model reductant, tin(II) chloride. The bioactivity of 1 was confirmed in antibacterial susceptibility assays whereas prodrug 2 was inactive.
中文翻译：
低氧激活的抗菌前药。
据报道，基于已知抗菌化合物的前药在还原条件下靶向金黄色葡萄球菌和大肠杆菌。前药是通过将赖氨酸残基的N端和侧链胺掩蔽为4-硝基苄基氨基甲酸酯来制备的。在用模型还原剂氯化锡（II）处理后，证明了释放出抗菌素的活化作用。在抗菌药敏试验中证实了1的生物活性，而前药2则没有活性。
更新日期：2020-04-20
中文翻译：
低氧激活的抗菌前药。
据报道，基于已知抗菌化合物的前药在还原条件下靶向金黄色葡萄球菌和大肠杆菌。前药是通过将赖氨酸残基的N端和侧链胺掩蔽为4-硝基苄基氨基甲酸酯来制备的。在用模型还原剂氯化锡（II）处理后，证明了释放出抗菌素的活化作用。在抗菌药敏试验中证实了1的生物活性，而前药2则没有活性。
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