Scaffold and Parasite Hopping : Discovery of New Protozoal Proliferation Inhibitors
Copyright © 2020 American Chemical Society..
Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
ACS medicinal chemistry letters - 11(2020), 3 vom: 12. März, Seite 249-257 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Singh, Baljinder [VerfasserIn] |
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| Anmerkungen: |
Date Revised 04.02.2022 published: Electronic-eCollection Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1021/acsmedchemlett.9b00453 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM307715035 |
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| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a Copyright © 2020 American Chemical Society. | ||
| 520 | |a Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria | ||
| 650 | 4 | |a Journal Article | |
| 700 | 1 | |a Bernatchez, Jean A |e verfasserin |4 aut | |
| 700 | 1 | |a McCall, Laura-Isobel |e verfasserin |4 aut | |
| 700 | 1 | |a Calvet, Claudia M |e verfasserin |4 aut | |
| 700 | 1 | |a Ackermann, Jasmin |e verfasserin |4 aut | |
| 700 | 1 | |a Souza, Julia M |e verfasserin |4 aut | |
| 700 | 1 | |a Thomas, Diane |e verfasserin |4 aut | |
| 700 | 1 | |a Silva, Everton M |e verfasserin |4 aut | |
| 700 | 1 | |a Bachovchin, Kelly A |e verfasserin |4 aut | |
| 700 | 1 | |a Klug, Dana M |e verfasserin |4 aut | |
| 700 | 1 | |a Jalani, Hitesh B |e verfasserin |4 aut | |
| 700 | 1 | |a Bag, Seema |e verfasserin |4 aut | |
| 700 | 1 | |a Buskes, Melissa J |e verfasserin |4 aut | |
| 700 | 1 | |a Leed, Susan E |e verfasserin |4 aut | |
| 700 | 1 | |a Roncal, Norma E |e verfasserin |4 aut | |
| 700 | 1 | |a Penn, Erica C |e verfasserin |4 aut | |
| 700 | 1 | |a Erath, Jessey |e verfasserin |4 aut | |
| 700 | 1 | |a Rodriguez, Ana |e verfasserin |4 aut | |
| 700 | 1 | |a Sciotti, Richard J |e verfasserin |4 aut | |
| 700 | 1 | |a Campbell, Robert F |e verfasserin |4 aut | |
| 700 | 1 | |a McKerrow, James |e verfasserin |4 aut | |
| 700 | 1 | |a Siqueira-Neto, Jair L |e verfasserin |4 aut | |
| 700 | 1 | |a Ferrins, Lori |e verfasserin |4 aut | |
| 700 | 1 | |a Pollastri, Michael P |e verfasserin |4 aut | |
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