含 3-烷氧基亚氨基-4-(环丙基亚氨基甲酰基)吡咯烷部分的氟喹诺酮衍生物的合成、抗分枝杆菌和抗菌活性。
Synthesis, antimycobacterial and antibacterial activity of fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety.
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China.
Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China.
出版信息
Eur J Med Chem. 2015 Nov 2;104:73-85. doi: 10.1016/j.ejmech.2015.09.030. Epub 2015 Sep 30.
A series of novel fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety were designed, synthesized and evaluated for their biological activity. Our results revealed that 19b2 shows good activity against MTB H37Rv ATCC 27294 (MIC: <0.25 μg/mL) and MDR-MTB 6133 clinical isolate (MIC: 0.11 μg/mL). Most of them have potent potency against Gram-positive strains, although they are generally poor active against Gram-negative strains. Especially, compounds 22b1 and 23a3 (MICs: <0.008-8 μg/mL) were found to 2-128 times more potent than ciprofloxacin and levofloxacin against all of the tested Gram-positive strains including quinolone-resistant MRSA, MRSE, Enterococcus faecium and Enterococcus faecalis.
设计、合成并评价了一系列含有 3-烷氧基亚氨基-4-(环丙基亚氨基)甲基吡咯烷部分的新型氟喹诺酮衍生物，用于研究其生物学活性。我们的结果表明，化合物 19b2 对结核分枝杆菌 H37Rv ATCC 27294（MIC：<0.25μg/mL）和耐多药结核分枝杆菌 6133 临床分离株（MIC：0.11μg/mL）具有良好的活性。它们大多数对革兰氏阳性菌株具有很强的活性，尽管它们通常对革兰氏阴性菌株的活性较差。特别是，化合物 22b1 和 23a3（MICs：<0.008-8μg/mL）对所有测试的革兰氏阳性菌株（包括耐喹诺酮的 MRSA、MRSE、粪肠球菌和屎肠球菌）的活性均比环丙沙星和左氧氟沙星强 2-128 倍。
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