去氢枞酸 N-磺氨乙基肟衍生物的合成及抗金葡菌活性。
The synthesis and antistaphylococcal activity of N-sulfonaminoethyloxime derivatives of dehydroabietic acid.
机构信息
Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
School of Life Sciences, Shanghai University, Shanghai 200444, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
出版信息
Bioorg Med Chem Lett. 2018 Jun 1;28(10):1943-1948. doi: 10.1016/j.bmcl.2018.03.062. Epub 2018 Mar 23.
A series of N-sulfonaminoethyloxime derivatives of dehydroabietic acid were synthesized and investigated for their antibacterial activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Most of the target compounds having chloro, bromo, trifluoromethyl phenyl moiety exhibited potent in vitro antistaphylococcal activity. The meta-CF phenyl derivative T23 showed the highest activity with MIC of 0.39-0.78 μg/mL against S. aureus Newman, while several analogues showed similar potent antibacterial activity with MIC values between 0.78 and 1.56 μg/mL against five multidrug-resistant S. aureus. The stability of T35 in plasma of SD rat and the cellular cytotoxicity were also evaluated.
一系列去氢枞酸 N-磺氨乙氧肟衍生物被合成并研究了它们对金黄色葡萄球菌新菌株和多药耐药菌株（NRS-1、NRS-70、NRS-100、NRS-108 和 NRS-271）的抗菌活性。大多数含有氯、溴、三氟甲基苯基部分的目标化合物表现出很强的体外抗葡萄球菌活性。间-CF 苯基衍生物 T23 对金黄色葡萄球菌 Newman 的活性最高，MIC 为 0.39-0.78μg/mL，而几个类似物对 5 株多药耐药的金黄色葡萄球菌的 MIC 值在 0.78-1.56μg/mL 之间，具有相似的强抗菌活性。还评估了 T35 在 SD 大鼠血浆中的稳定性和细胞毒性。
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