Exploring a Tetrahydroquinoline Antimalarial Hit from the Medicines for Malaria Pathogen Box and Identification of its Mode of Resistance as PfeEF2,ChemMedChem

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Exploring a Tetrahydroquinoline Antimalarial Hit from the Medicines for Malaria Pathogen Box and Identification of its Mode of Resistance as PfeEF2
ChemMedChem ( IF 3.4 ) Pub Date : 2022-09-21 , DOI: 10.1002/cmdc.202200393
Benoît Laleu ₁ , Kelly Rubiano _{2,

3} , Tomas Yeo ₂ , Irene Hallyburton ₄ , Mark Anderson ₄ , Benigno Crespo-Fernandez ₅ , Francisco-Javier Gamo ₅ , Yevgeniya Antonova-Koch _{6,

7} , Pamela Orjuela-Sanchez _{6,

8} , Sergio Wittlin _{9,

10} , Gouranga P Jana ₁₁ , Bikash C Maity ₁₁ , Elodie Chenu ₁ , James Duffy ₁ , Peter Sjö ₁ , David Waterson ₁ , Elizabeth Winzeler ₆ , Eric Guantai ₁₂ , David A Fidock _{2,

13} , Thomas G Hansson ₁

Affiliation

Medicines for Malaria Venture, International Centre Cointrin, Route de Pré-Bois 20, P.O. Box 1826, 1215, Geneva 15, Switzerland.
Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY, 10032, USA.
Current address, Department of Molecular Microbiology, Washington University School of Medicine, Saint Louis, MO, 63110, USA.
Drug Discovery Unit, Wellcome Centre for Anti-infective Research, University of Dundee, Dow Street, Dundee, DD1 5EH, UK.
Global Health, GlaxoSmithKline R&D, Tres Cantos, 28760, Madrid, Spain.
Department of Pediatrics, School of Medicine, University of California San Diego, La Jolla, CA, 92093, USA.
Current address, Calibr, A Division of Scripps Research, 11119 North Torrey Pines Road, La Jola, CA, 92037, USA.
Current address, Novartis Institute for Tropical Diseases, 5959 Horton Street, 8th floor, Emeryville, CS, 94608, USA.
Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002, Basel, Switzerland.
University of Basel, 4002, Basel, Switzerland.
TCG Lifesciences Private Limited, Block BN, Plot 7 Salt-lake Electronics Complex, Sector V, Kolkata, 700091, West Bengal, India.
Department of Pharmacy, Faculty of Health Sciences, University of Nairobi, 00202-, Nairobi, Kenya.
Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, NY, 10032, USA.

Toolkit expansion: We report an exploration of the antimalarial compound MMV692140. The mode of resistance was identified as PfeEF2. The structural motif was explored in a chemistry program, resulting in the identification of MMV1919557, an analog with significantly improved antimalarial potency. This new series could provide a tool to further understand the potential of PfeEF2 as a target for malaria treatment.

中文翻译：

从疟疾病原体药物盒中探索四氢喹啉类抗疟药及其耐药模式鉴定为 PfeEF2

工具包扩展：我们报告了抗疟化合物 MMV692140 的探索。耐药模式被确定为Pf eEF2。在化学程序中探索了结构基序，从而鉴定出 MMV1919557，这是一种抗疟药效显着提高的类似物。这个新系列可以提供一种工具，以进一步了解Pf eEF2 作为疟疾治疗靶标的潜力。

更新日期：2022-09-21

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