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Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
Visceral leishmaniasis (VL) affects millions of people across the world, largely in developing nations. It is fatal if left untreated and the current treatments are inadequate. As such, there is an urgent need for new, improved medicines. In this paper, we describe the identification of a 6-amino-N-...
| Autores principales: | , , , , , , , , , , , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Royal Society of Chemistry
2020
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7651859/ https://www.ncbi.nlm.nih.gov/pubmed/33479621 http://dx.doi.org/10.1039/d0md00203h |
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| author | Thomas, Michael G. De Rycker, Manu Ajakane, Myriam Crouch, Sabrinia D. Campbell, Lorna Daugan, Alain Fra, Gloria Guerrero, César Mackenzie, Claire J. MacLean, Lorna Manthri, Sujatha Martin, Franck Norval, Suzanne Osuna-Cabello, Maria Riley, Jennifer Shishikura, Yoko Miguel-Siles, Juan Simeons, Frederick R. C. Stojanovski, Laste Thomas, John Thompson, Stephen Velasco, Raul F. Fiandor, Jose M. Wyatt, Paul G. Read, Kevin D. Gilbert, Ian H. Miles, Timothy J. |
| author_facet | Thomas, Michael G. De Rycker, Manu Ajakane, Myriam Crouch, Sabrinia D. Campbell, Lorna Daugan, Alain Fra, Gloria Guerrero, César Mackenzie, Claire J. MacLean, Lorna Manthri, Sujatha Martin, Franck Norval, Suzanne Osuna-Cabello, Maria Riley, Jennifer Shishikura, Yoko Miguel-Siles, Juan Simeons, Frederick R. C. Stojanovski, Laste Thomas, John Thompson, Stephen Velasco, Raul F. Fiandor, Jose M. Wyatt, Paul G. Read, Kevin D. Gilbert, Ian H. Miles, Timothy J. |
| author_sort | Thomas, Michael G. |
| collection | PubMed |
| description | Visceral leishmaniasis (VL) affects millions of people across the world, largely in developing nations. It is fatal if left untreated and the current treatments are inadequate. As such, there is an urgent need for new, improved medicines. In this paper, we describe the identification of a 6-amino-N-(piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine scaffold and its optimization to give compounds which showed efficacy when orally dosed in a mouse model of VL. |
| format | Online Article Text |
| id | pubmed-7651859 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2020 |
| publisher | Royal Society of Chemistry |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-76518592020-11-17 Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis Thomas, Michael G. De Rycker, Manu Ajakane, Myriam Crouch, Sabrinia D. Campbell, Lorna Daugan, Alain Fra, Gloria Guerrero, César Mackenzie, Claire J. MacLean, Lorna Manthri, Sujatha Martin, Franck Norval, Suzanne Osuna-Cabello, Maria Riley, Jennifer Shishikura, Yoko Miguel-Siles, Juan Simeons, Frederick R. C. Stojanovski, Laste Thomas, John Thompson, Stephen Velasco, Raul F. Fiandor, Jose M. Wyatt, Paul G. Read, Kevin D. Gilbert, Ian H. Miles, Timothy J. RSC Med Chem Chemistry Visceral leishmaniasis (VL) affects millions of people across the world, largely in developing nations. It is fatal if left untreated and the current treatments are inadequate. As such, there is an urgent need for new, improved medicines. In this paper, we describe the identification of a 6-amino-N-(piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine scaffold and its optimization to give compounds which showed efficacy when orally dosed in a mouse model of VL. Royal Society of Chemistry 2020-08-06 /pmc/articles/PMC7651859/ /pubmed/33479621 http://dx.doi.org/10.1039/d0md00203h Text en This journal is © The Royal Society of Chemistry 2020 http://creativecommons.org/licenses/by/3.0/ This article is freely available. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence (CC BY 3.0) |
| spellingShingle | Chemistry Thomas, Michael G. De Rycker, Manu Ajakane, Myriam Crouch, Sabrinia D. Campbell, Lorna Daugan, Alain Fra, Gloria Guerrero, César Mackenzie, Claire J. MacLean, Lorna Manthri, Sujatha Martin, Franck Norval, Suzanne Osuna-Cabello, Maria Riley, Jennifer Shishikura, Yoko Miguel-Siles, Juan Simeons, Frederick R. C. Stojanovski, Laste Thomas, John Thompson, Stephen Velasco, Raul F. Fiandor, Jose M. Wyatt, Paul G. Read, Kevin D. Gilbert, Ian H. Miles, Timothy J. Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis |
| title | Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
|
| title_full | Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
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| title_fullStr | Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
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| title_full_unstemmed | Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
|
| title_short | Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
|
| title_sort | identification of 6-amino-1h-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis |
| topic | Chemistry |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7651859/ https://www.ncbi.nlm.nih.gov/pubmed/33479621 http://dx.doi.org/10.1039/d0md00203h |
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