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Chang-Ji Zheng#, Ming-Xia Song#, Liang-Peng Sun, Yan Wu, Lan Hong, Hu-Ri Piao*. Synthesis and biological evaluation of 5-aryloxypyrazole derivatives bearing a rhodanine-3-aromatic acid as potential antimicrobial agents. Bioorg Med Chem Lett. 22(23), 7024¨C7028, 2012
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The synthesis and SAR study of phenylalanine-derived (Z)-5-arylmethylidene rhodanines as anti-methicillin-resistant Staphylococcus aureus (MRSA) compounds

×÷Õß: Patel, Bhargav A.; Ashby, Charles R., Jr.; Hardej, Diane; µÈ.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS  ¾í: 23   ÆÚ: 20   Ò³: 5523-5527   ³ö°æÄê: OCT 15 2013

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Synthesis and X-ray structure characterisation of novel pyrazole carboxamide derivatives

×÷Õß: Lv, Hong-Shui; Ding, Xiao-Ling; Zhao, Bao-Xiang

JOURNAL OF CHEMICAL RESEARCH  ÆÚ: 4   Ò³: 223-226   ³ö°æÄê: APR 2013

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dengxianqing: ½ð±Ò+2 2014-09-20 16:42:02
Synthesis and biological evaluation of 5-aryloxypyrazole derivatives bearing a rhodanine-3-aromatic acid as potential antimicrobial agents


×÷Õß:Zheng, CJ (Zheng, Chang-Ji)[ 1 ] ; Song, MX (Song, Ming-Xia)[ 1 ] ; Sun, LP (Sun, Liang-Peng)[ 1 ] ; Wu, Y (Wu, Yan)[ 1 ] ; Hong, L (Hong, Lan)[ 2 ] ; Piao, HR (Piao, Hu-Ri)[ 1 ]




BIOORGANIC & MEDICINAL CHEMISTRY LETTERS



¾í: 22

ÆÚ: 23

Ò³: 7024-7028

DOI: 10.1016/j.bmcl.2012.09.107

³ö°æÄê: DEC 1 2012

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Three novel series of 5-aryloxypyrazole derivatives have been synthesized and tested for their antibacterial activity. The majority of the synthesized compounds showed potent inhibitory activity against Gram-positive bacteria Staphylococcus aureus 4220, especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compounds IIIb, IIIg and IIIm showed the most potent levels of activity (MIC = 1 mu g/mL) against the multidrug-resistant strains. And cytotoxic activity assay showed that the compounds tested did not affect cell viability on the Human cervical (HeLa) cells at their MICs. The current study therefore suggests that 5-aryloxypyrazoles bearing a rhodanine-3-aromatic acid moiety are promising scaffolds for the development of novel Gram-positive antibacterial agents. (C) 2012 Elsevier Ltd. All rights reserved.


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×÷Õ߹ؼü´Ê:Rhodanine; 5-Aryloxypyrazole; Antibacterial activity

KeyWords PlusYRAZOLE-RELATED NUCLEOSIDES; ANTITUMOR-ACTIVITY; ANTIBACTERIAL ACTIVITY; INHIBITORS; 4-THIAZOLIDINONE; IDENTIFICATION; ANTIFUNGAL; DESIGN; ETHERS; MICE


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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, Yanji 133002, 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, Peoples R China







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





µç×ÓÓʼþµØÖ·:piaohuri@yahoo.com.cn


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National Science Foundation of China


20962021

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PERGAMON-ELSEVIER SCIENCE LTD, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND


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Ñо¿·½Ïòharmacology & Pharmacy; Chemistry

Web of Science Àà±ð:Chemistry, Medicinal; Chemistry, Organic


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ÎÄÏ×ÀàÐÍ:Article

ÓïÖÖ:English

Èë²ØºÅ: WOS:000310583100005

ISSN: 0960-894X


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Impact Factor (Ó°ÏìÒò×Ó): Journal Citation Reports®


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IDS ºÅ: 030PR

Web of Science ºËÐĺϼ¯ÖÐµÄ "ÒýÓõIJο¼ÎÄÏ×": 30

Web of Science ºËÐĺϼ¯ÖÐµÄ "±»ÒýƵ´Î": 2
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2Â¥: Originally posted by baiyuefei at 2014-09-20 12:03:34
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The synthesis and SAR study of phenylalanine-derived (Z)-5-arylmethylidene rhodanines as anti-methicillin-resistant Staphylococcus aureus (MRSA) compounds

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