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ÂÛÎÄÏêϸÐÅÏ¢ÈçÏ£ºMing-Xia Song, Chang-Ji Zheng, Liang-Peng Sun, Yan Wu, Lan Hong, Ying-Jing Li, Yi Liu, Zhi-Yu Wei, Ming-Jun Jin, Hu-Ri Piao*. Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA). Eur J Med Chem. 60, 376-385, 2013.
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Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA)


×÷Õß:Song, MX (Song, Ming-Xia)[ 1,2 ] ; Zheng, CJ (Zheng, Chang-Ji)[ 1 ] ; Deng, XQ (Deng, Xian-Qing)[ 1 ] ; Sun, LP (Sun, Liang-Peng)[ 1 ] ; Wu, Y (Wu, Yan)[ 1 ] ; Hong, L (Hong, Lan)[ 3 ] ; Li, YJ (Li, Ying-Jing)[ 1 ] ; Liu, Y (Liu, Yi)[ 1 ] ; Wei, ZY (Wei, Zhi-Yu)[ 1 ] ; Jin, MJ (Jin, Ming-Jun)[ 1 ] ¸ü¶àÄÚÈÝ




EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY



¾í: 60

Ò³: 376-385

DOI: 10.1016/j.ejmech.2012.12.007

³ö°æÄê: FEB 2013

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With an intention to synergize the anti-bacterial activity of 5-aryloxy pyrazole and rhodanine derivatives, eight series of hybrid compounds have been synthesized and evaluated for their antibacterial activity. The majority of the synthesized compounds showed good inhibitory activity against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA, QRSA) with minimum inhibitory concentration (MIC) values in the range of 1-32 mu g/mL. The cytotoxicity test suggests that these compounds exhibited in vitro antibacterial activity at non-cytotoxic concentrations. These studies therefore suggest that rhodanine-based 5-aryloxy pyrazoles are interesting scaffolds for the development of novel Gram-positive antibacterial agents. (C) 2012 Elsevier Masson SAS. All rights reserved.


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×÷Õ߹ؼü´Ê:Rhodanine; 5-Aryloxy pyrazole; Anti-bacterial; MRSA; QRSA

KeyWords PlusERIVATIVES; 4-THIAZOLIDINONE; AGENTS


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ͨѶ×÷ÕßµØÖ·: Piao, HR (ͨѶ×÷Õß)





Yanbian Univ, Coll Pharm, Affiliated Minist Educ, Key Lab Nat Resources & Funct Mol Changbai Mt, 977 Gongyuan Rd, Yanji 133002, Jilin, Peoples R China.





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[ 1 ] Yanbian Univ, Coll Pharm, Affiliated Minist Educ, Key Lab Nat Resources & Funct Mol Changbai Mt, Yanji 133002, Jilin, Peoples R China





      

[ 2 ] Jinggangshan Univ, Coll Med, Jian 343100, Jiangxi, Peoples R China





[ 3 ] Yanbian Univ, Coll Med, Yanji 133002, Jilin, Peoples R China





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National Science Foundation of China


20962021

81260468

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