Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.

Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
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DOI:
10.1016/j.bmcl.2010.11.102
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发表时间:
2010-06
影响因子:
2.7
通讯作者:
W. Shi;Haikun Ma;Yuejiao Duan;Kelly M. Aubart;Yuhong Fang;Rimma Zonis;Liping Yang;Wenhao Hu
W. Shi;Haikun Ma;Yuejiao Duan;Kelly M. Aubart;Yuhong Fang;Rimma Zonis;Liping Yang;Wenhao Hu
中科院分区:
医学4区
文献类型:
--
作者:
W. Shi;Haikun Ma;Yuejiao Duan;Kelly M. Aubart;Yuhong Fang;Rimma Zonis;Liping Yang;Wenhao Hu

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报道了3-亚甲基吡咯烷甲酰基羟氨基衍生物的合成及其抑菌活性。对这些衍生物的抗菌活性进行了评估,发现了p1 ‘和p3 ’位置的SAR,并且大多数这些衍生物对耐药临床分离株(包括MRSA, PRSP和流感嗜血杆菌)的体外抗菌活性优于现有药物。
The synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated to discover SAR at P1′and P3′positions, and most of these derivatives exhibit better in vitro antibacterial activity than existing drugs against drug-resistant clinical isolates including MRSA, PRSP, and Haemophilus influenzae.