Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferase

被引：56

作者：

Rackham, Mark D. ^{[1
]}

Brannigan, James A. ^{[2
]}

Moss, David K. ^{[3
]}

Yu, Zhiyong ^{[1
]}

Wilkinson, Anthony J. ^{[2
]}

Holder, Anthony A. ^{[3
]}

Tate, Edward W. ^{[1
]}

Leatherbarrow, Robin J. ^{[1
]}

机构：

[1] Univ London Imperial Coll Sci Technol & Med, Dept Chem, London SW7 2AZ, England

[2] Univ York, Dept Chem, York Struct Biol Lab, York YO10 5DD, N Yorkshire, England

[3] MRC Natl Inst Med Res, Div Parasitol, London NW7 1AA, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 56卷 / 01期

基金：

英国医学研究理事会; 英国工程与自然科学研究理事会; 英国生物技术与生命科学研究理事会;

关键词：

DESIGN;

D O I：

10.1021/jm301474t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Myristoyltransferase (NMT) is an attractive antiprotozoan drug target. A lead-hopping approach was utilized in the design and synthesis of novel benzo[b]thiophene-containing inhibitors of Plasmodium falciparum (PO and Plasmodium vivax (Pv) NMT. These inhibitors are selective against Homo sapiens NMT1 (HsNMT), have excellent ligand efficiency (LE), and display antiparasitic activity in vitro. The binding mode of this series was determined by crystallography and shows a novel binding mode for the benzothiophene ring.

引用

页码：371 / 375

页数：5

共 50 条

[41] Identification of Novel Plasmodium falciparum Hexokinase Inhibitors with Antiparasitic Activity
Davis, Mindy I.
Patrick, Stephen L.
Blanding, Walker M.
Dwivedi, Varun
Suryadi, Jimmy
Golden, Jennifer E.
Coussens, Nathan P.
Lee, Olivia W.
Shen, Min
Boxer, Matthew B.
Hall, Matthew D.
Sharlow, Elizabeth R.
Drew, Mark E.
Morris, James C.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2016, 60 (10) : 6023 - 6033
[42] Computational Design of Novel Allosteric Inhibitors for Plasmodium falciparum DegP
Shehzad, Sadaf
Pandey, Rajan
Malhotra, Pawan
Gupta, Dinesh
MOLECULES, 2021, 26 (09):
[43] A novel real-time PCR assay for the detection of Plasmodium falciparum and Plasmodium vivax malaria in low parasitized individuals
Hwang, Seung-Young
Kim, So-Hee
Lee, Ga-Young
Vu Thi Thu Hang
Moon, Chi-Sook
Shin, Jeong Hwan
Koo, Wan-Lim
Kim, Seong-Youl
Park, Hae-Joon
Park, Han-Oh
Kho, Weon-Gyu
ACTA TROPICA, 2011, 120 (1-2) : 40 - 45
[44] Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes
Bell, Andrew S.
Yu, Zhiyong
Hutton, Jennie A.
Wright, Megan H.
Brannigan, James A.
Paape, Daniel
Roberts, Shirley M.
Sutherell, Charlotte L.
Ritzefeld, Markus
Wilkinson, Anthony J.
Smith, Deborah F.
Leatherbarrow, Robin J.
Tate, Edward W.
JOURNAL OF MEDICINAL CHEMISTRY, 2020, 63 (14) : 7740 - 7765
[45] A novel in vitro model reveals distinctive modulatory roles of Plasmodium falciparum and Plasmodium vivax on naive cell-mediated immunity
Chitsanoor, Setthakit
Somsri, Sangdao
Panburana, Panyu
Mungthin, Mathirut
Ubalee, Ratawan
Emyeam, Maliwan
Jongwutiwes, Somchai
Sattabongkot, Jetsumon
Udomsangpetch, Rachanee
MALARIA JOURNAL, 2017, 16
[46] Discovery of Ligand-Efficient Scaffolds for the Design of Novel Trichomonas vaginalis Uridine Nucleoside Ribohydrolase Inhibitors Using Fragment Screening
Auletta, Shannon
Caravan, Wagma
Persaud, Julia K.
Thuilot, Samantha F.
Brown, Dean G.
Parkin, David W.
Stockman, Brian J.
ACS OMEGA, 2019, 4 (14): : 16226 - 16232
[47] Design of Novel Dihydroxynaphthoic Acid Inhibitors of Plasmodium Falciparum Lactate Dehydrogenase
Megnassan, Eugene
Keita, Melalie
Bieri, Cecile
Esmel, Akori
Frecer, Vladimir
Miertus, Stanislav
MEDICINAL CHEMISTRY, 2012, 8 (05) : 970 - 984
[48] Designing novel inhibitors against falcipain-2 of Plasmodium falciparum
Himangini
Pathak, Dharam Pal
Sharma, Vidushi
Kumar, Sachin
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (09) : 1566 - 1569
[49] In silico identification of novel inhibitors against Plasmodium falciparum dihydroorate dehydrogenase
Wadood, Abdul
Ul-Haq, Zaheer
JOURNAL OF MOLECULAR GRAPHICS & MODELLING, 2013, 40 : 40 - 47
[50] Synthesis of novel α-pyranochalcones and pyrazoline derivatives as Plasmodium falciparum growth inhibitors
Wanare, Gajanan
Aher, Rahul
Kawathekar, Neha
Ranjan, Ravi
Kaushik, Naveen Kumar
Sahal, Dinkar
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (15) : 4675 - 4678

← 1 2 3 4 5 →