Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
Тип публикации: Journal Article
Дата публикации: 2021-02-12
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.1
Impact factor: 7.3
ISSN: 00222623, 15204804
PubMed ID:
33573376
Drug Discovery
Molecular Medicine
Краткое описание
A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp3-rich scaffold provided an attractive starting point for a hit-to-lead medicinal chemistry optimization and biological profiling program. Structure-activity-relationship studies led to the identification of compounds that showed low nanomolar asexual blood-stage activity (<50 nM) together with strong gametocyte sterilizing properties that translated to transmission-blocking activity in the standard membrane feeding assay. Mechanistic studies through resistance selection with one of the analogues followed by whole-genome sequencing implicated the P. falciparum cyclic amine resistance locus in the mode of resistance.
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ГОСТ
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Le Manach C. et al. Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts // Journal of Medicinal Chemistry. 2021. Vol. 64. No. 4. pp. 2291-2309.
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Le Manach C. et al. Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts // Journal of Medicinal Chemistry. 2021. Vol. 64. No. 4. pp. 2291-2309.
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TY - JOUR
DO - 10.1021/acs.jmedchem.1c00034
UR - https://doi.org/10.1021/acs.jmedchem.1c00034
TI - Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
T2 - Journal of Medicinal Chemistry
AU - Le Manach, Claire
AU - Dam, Jean
AU - Woodland, John G
AU - Kaur, Gurminder
AU - Khonde, Lutete P
AU - Brunschwig, Christel
AU - Njoroge, Mathew
AU - Wicht, Kathryn J.
AU - Horatscheck, Andre
AU - Paquet, Tanya
AU - Boyle, Grant A.
AU - Gibhard, Liezl
AU - Taylor, Dale L.
AU - Lawrence, Nina
AU - Yeo, Tomas
AU - Mok, Sachel
AU - Eastman, Richard
AU - Dorjsuren, Dorjbal
AU - Talley, Daniel C.
AU - Guo, Hui
AU - Simeonov, Anton
AU - Reader, Janette
AU - Van Der Watt, Mariëtte E
AU - Erlank, Erica
AU - Venter, Nelius
AU - Zawada, Jacek W
AU - Aswat, Ayesha
AU - Nardini, Luisa
AU - Coetzer, Thérèsa L.
AU - Lauterbach, Sonja
AU - Bezuidenhout, Belinda C
AU - Theron, Anjo
AU - Mancama, Dalu
AU - Koekemoer, Lizette L.
AU - Birkholtz, L.
AU - Wittlin, Sergio
AU - Delves, Michael
AU - Ottilie, Sabine
AU - Winzeler, Elizabeth A.
AU - von Geldern, Thomas W
AU - Smith, Dennis
AU - Fidock, David A.
AU - Street, Leslie J
AU - Basarab, Gregory S.
AU - Duffy, James E S
AU - Chibale, Kelly
PY - 2021
DA - 2021/02/12
PB - American Chemical Society (ACS)
SP - 2291-2309
IS - 4
VL - 64
PMID - 33573376
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (до 50 авторов)
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@article{2021_Le Manach,
author = {Claire Le Manach and Jean Dam and John G Woodland and Gurminder Kaur and Lutete P Khonde and Christel Brunschwig and Mathew Njoroge and Kathryn J. Wicht and Andre Horatscheck and Tanya Paquet and Grant A. Boyle and Liezl Gibhard and Dale L. Taylor and Nina Lawrence and Tomas Yeo and Sachel Mok and Richard Eastman and Dorjbal Dorjsuren and Daniel C. Talley and Hui Guo and Anton Simeonov and Janette Reader and Mariëtte E Van Der Watt and Erica Erlank and Nelius Venter and Jacek W Zawada and Ayesha Aswat and Luisa Nardini and Thérèsa L. Coetzer and Sonja Lauterbach and Belinda C Bezuidenhout and Anjo Theron and Dalu Mancama and Lizette L. Koekemoer and L. Birkholtz and Sergio Wittlin and Michael Delves and Sabine Ottilie and Elizabeth A. Winzeler and Thomas W von Geldern and Dennis Smith and David A. Fidock and Leslie J Street and Gregory S. Basarab and James E S Duffy and Kelly Chibale and others},
title = {Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts},
journal = {Journal of Medicinal Chemistry},
year = {2021},
volume = {64},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://doi.org/10.1021/acs.jmedchem.1c00034},
number = {4},
pages = {2291--2309},
doi = {10.1021/acs.jmedchem.1c00034}
}
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MLA
Скопировать
Le Manach, Claire, et al. “Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.” Journal of Medicinal Chemistry, vol. 64, no. 4, Feb. 2021, pp. 2291-2309. https://doi.org/10.1021/acs.jmedchem.1c00034.
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