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

页码：191 / 197

页数：7

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