Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase

被引：13
|
作者：
Goncalves, Victor [1 ,3 ]
Brannigan, James A. [2 ]
Laporte, Alice [1 ]
Bell, Andrew S. [1 ]
Roberts, Shirley M. [2 ]
Wilkinson, Anthony J. [2 ]
Leatherbarrow, Robin J. [1 ,4 ]
Tate, Edward W. [1 ]
机构：
[1] Imperial Coll London, Dept Chem, London SW7 2AZ, England
[2] Univ York, Dept Chem, Struct Biol Lab, York YO10 5DD, N Yorkshire, England
[3] Univ Bourgogne Franche Comte, ICMUB, F-21000 Dijon, France
[4] Liverpool John Moores Univ, Egerton Court,2 Rodney St, Liverpool L1 2UA, Merseyside, England
来源：
MEDCHEMCOMM | 2017年 / 8卷 / 01期
基金：
英国医学研究理事会; 英国惠康基金; 英国工程与自然科学研究理事会;
关键词：
POTENTIAL-DRUG TARGET; MYRISTOYL-COA; SELECTIVE INHIBITORS; VIVAX MALARIA; DISCOVERY; DESIGN; LIGAND; LEISHMANIASIS; FALCIPARUM; PARASITES;
D O I：
10.1039/c6md00531d
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The parasite Plasmodium vivax is the most widely distributed cause of recurring malaria. N-Myristoyltransferase (NMT), an enzyme that catalyses the covalent attachment of myristate to the N-terminal glycine of substrate proteins, has been described as a potential target for the treatment of this disease. Herein, we report the synthesis and the structure-guided optimization of a series of quinolines with balanced activity against both Plasmodium vivax and Plasmodium falciparum N-myristoyltransferase (NMT).
引用
收藏
页码：191 / 197
页数：7
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