Anilinoquinoline based inhibitors of trypanosomatid proliferation
We recently reported the medicinal chemistry re-optimization of a series of compounds derived from the human tyrosine kinase inhibitor, lapatinib, for activity against Plasmodium falciparum. From this same library of compounds, we now report potent compounds against Trypanosoma brucei brucei (which causes human African trypanosomiasis), T. cruzi (the pathogen that causes Chagas disease), and Leishmania spp. (which cause leishmaniasis). In addition, sub-micromolar compounds were identified that inhibit proliferation of the parasites that cause African animal trypanosomiasis, T. congolense and T. vivax. We have found that this set of compounds display acceptable physicochemical properties and represent progress towards identification of lead compounds to combat several neglected tropical diseases.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
PLoS neglected tropical diseases - 12(2018), 11 vom: 26. Nov., Seite e0006834 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ferrins, Lori [VerfasserIn] |
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| Links: |
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| Themen: |
2-anilino-5-thiazolinone |
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| Anmerkungen: |
Date Completed 21.01.2019 Date Revised 09.03.2020 published: Electronic-eCollection Citation Status MEDLINE |
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| doi: |
10.1371/journal.pntd.0006834 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM291071082 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a We recently reported the medicinal chemistry re-optimization of a series of compounds derived from the human tyrosine kinase inhibitor, lapatinib, for activity against Plasmodium falciparum. From this same library of compounds, we now report potent compounds against Trypanosoma brucei brucei (which causes human African trypanosomiasis), T. cruzi (the pathogen that causes Chagas disease), and Leishmania spp. (which cause leishmaniasis). In addition, sub-micromolar compounds were identified that inhibit proliferation of the parasites that cause African animal trypanosomiasis, T. congolense and T. vivax. We have found that this set of compounds display acceptable physicochemical properties and represent progress towards identification of lead compounds to combat several neglected tropical diseases | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Sharma, Amrita |e verfasserin |4 aut | |
| 700 | 1 | |a Thomas, Sarah M |e verfasserin |4 aut | |
| 700 | 1 | |a Mehta, Naimee |e verfasserin |4 aut | |
| 700 | 1 | |a Erath, Jessey |e verfasserin |4 aut | |
| 700 | 1 | |a Tanghe, Scott |e verfasserin |4 aut | |
| 700 | 1 | |a Leed, Susan E |e verfasserin |4 aut | |
| 700 | 1 | |a Rodriguez, Ana |e verfasserin |4 aut | |
| 700 | 1 | |a Mensa-Wilmot, Kojo |e verfasserin |4 aut | |
| 700 | 1 | |a Sciotti, Richard J |e verfasserin |4 aut | |
| 700 | 1 | |a Gillingwater, Kirsten |e verfasserin |4 aut | |
| 700 | 1 | |a Pollastri, Michael P |e verfasserin |4 aut | |
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