Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents
Article
Peres, Raiza Brandão, Ullah, Asma Inam, de Almeida Fiuza, Ludmila Ferreira, Silva, Patricia Bernardino, Batista, Marcos M., Corcoran, O., Reddy, T. and de Nazaré Correia Soeiro, Maria 2018. Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents. Bioorganic & Medicinal Chemistry Letters. 28 (11), pp. 2018-2022. https://doi.org/10.1016/j.bmcl.2018.04.064
| Authors | Peres, Raiza Brandão, Ullah, Asma Inam, de Almeida Fiuza, Ludmila Ferreira, Silva, Patricia Bernardino, Batista, Marcos M., Corcoran, O., Reddy, T. and de Nazaré Correia Soeiro, Maria |
|---|---|
| Abstract | Chagas disease is a neglected pathology responsible for about 12,000 deaths every year across Latin America. Although six million people are infected by the Trypanosoma cruzi, current therapeutic options are limited, highlighting the need for new drugs. Here we report the preliminary structure activity relationships of a small library of 17 novel pyridyl sulfonamide derivatives. Analogues 4 and 15 displayed significant potency against intracellular amastigotes with EC50 of 5.4 µM and 8.6 µM. In cytotoxicity assays using mice fibroblast L929 cell lines, both compounds indicated low toxicity with decent selectivity indices (SI) >36 and >23 respectively. Hence these compounds represent good starting points for further lead optimization. |
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Journal citation | 28 (11), pp. 2018-2022 |
| ISSN | 0960-894X |
| Year | 2018 |
| Publisher | Elsevier |
| Accepted author manuscript | License |
| Accepted author manuscript | License |
| Digital Object Identifier (DOI) | https://doi.org/10.1016/j.bmcl.2018.04.064 |
| Web address (URL) | https://doi.org/10.1016/j.bmcl.2018.04.064 |
| Publication dates | |
| Online | 30 Apr 2018 |
| 15 Jun 2018 | |
| Publication process dates | |
| Deposited | 29 May 2018 |
| Accepted | 27 Apr 2018 |
| Accepted | 27 Apr 2018 |
| Funder | Fundação Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ) |
| Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) | |
| Fundação Oswaldo Cruz | |
| PTDIS | |
| PAEF/CNPq/Fiocruz CAPES | |
| University of East London | |
| Copyright information | © 2018 Elsevier |
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Accepted author manuscript
| Sulfonamides_manuscript_submitted.pdf | ||
| License: CC BY-NC-ND 4.0 | ||
| Sulfonamides_Supporting Information.pdf | ||
| License: CC BY-NC-ND 4.0 | ||
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