Design,synthesis and bioevaluation of N-hydroxyquinolinones as potential anti-plasmodial,anti-bacterial and iron(Ⅱ)-chelating agents

作     者：Yan-boTENG AliceSoh-MeoyONG LaurentRNIA ChristinaLi-LinCHAI 

作者机构：Department of Pharmacy National University of Singapore 18 Science Drive 4 117543 Laboratory of Malaria Immunobiology Singapore Immunology Network (SIgN) Agency for Science Technology and Research (A*STAR) 8ABiomedical Grove Immunos Building 138648 Singapore Institute of Chemical and Engineering Sciences (ICES) Agency for Science Technology and Research (A*STAR) 8 Biomedical Grove 138665 Singapore 

出 版 物：《中国药理学与毒理学杂志》 (Chinese Journal of Pharmacology and Toxicology)

年 卷 期：2015年第29卷第S1期

页      面：101-101页

核心收录：

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

基　　金：The project supported by the Agency for Science Technology and Research(A*STAR)(JCO-10/03/FG/06/02) 

主　　题：N-hydroxyquinolinones anti-plasmodial anti-bacteri 

摘      要：OBJECTIVE To establish a small compound library via a versatile synthetic route for the investigation of natural-inspiring compounds containing N-hydroxypyridones motif as potential anti-plasmodial,anti-bacterial and iron(Ⅱ)-chelating *** An amidation/cyclization approach was adopted to synthesize a library of *** anti-plasmodial susceptibility of lab clone 3D7 *** was measured using aprotocol modified from the WHO *** minimum bactericidal concentration(MBC)values were determined against Escherichia coli and Staphylococcus *** compounds were selected to test their iron(Ⅱ)-chelating *** iron(Ⅱ)-chelating ability was determined by measuring the absorbance of ferrozine-iron complex at 562 *** A new route for the facile synthesis of a library of N-hydroxyquinolinones based on one-pot palladium catalyzed C-N amidation/dehydrocyclizationsequence was *** compounds show anti-plasmodial activities with the range of 1.1-1.4μmol·L-1,50% chelation abilities of the nine selected compounds were shown to be 0.24-0.29mmol·*** Alibrary of N-hydroxyquinolinones was synthesized via a novel synthetic *** anti-plasmodial and anti-bacterial activities of these compounds were *** compounds show potent anti-plasmodial activities Nine compounds were examined for their propensities to undergo iron chelation and these compounds were shown to be promising iron(Ⅱ)chelators as compared to EDTA.