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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Synthesis and Structure-Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases

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Author(s):
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Silva, Daniel G. [1, 2] ; Junker, Anna [2] ; de Melo, Shaiani M. G. [1] ; Fumagalli, Fernando [3] ; Gillespie, J. Robert [4] ; Molasky, Nora [4] ; Buckner, Frederick S. [4] ; Matheeussen, An [5] ; Caljon, Guy [5] ; Maes, Louis [5] ; Emery, Flavio S. [1]
Total Authors: 11
Affiliation:
[1] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, QHeteM Lab Quim Heterocicl & Med, BR-14040903 Ribeirao Preto, SP - Brazil
[2] Westphalian Wilhelms Univ, European Inst Mol Imaging EIMI, D-48149 Munster - Germany
[3] Univ Fed Santa Maria UFSM, Ctr Ciencias Saude CCS, Av Roraima 1000, BR-97105900 Santa Maria, RS - Brazil
[4] Univ Washington, Dept Med, Seattle, WA 98195 - USA
[5] Univ Antwerp, Lab Microbiol Parasitol & Hyg LMPH, Univ Pl 1, B-2610 Antwerp - Belgium
Total Affiliations: 5
Document type: Journal article
Source: CHEMMEDCHEM; v. 16, n. 6 NOV 2020.
Web of Science Citations: 0
Abstract

Neglected tropical diseases remain among the most critical public health concerns in Africa and South America. The drug treatments for these diseases are limited, which invariably leads to fatal cases. Hence, there is an urgent need for new antitrypanosomal drugs. To address this issue, a large number of diverse heterocyclic compounds were prepared. Straightforward synthetic approaches tolerated pre-functionalized structures, giving rise to a structurally diverse set of analogs. We report on a set of 57 heterocyclic compounds with selective activity potential against kinetoplastid parasites. In general, 29 and 19 compounds of the total set could be defined as active against Trypanosoma cruzi and T. brucei brucei, respectively (antitrypanosomal activities <10 mu M). The present work discusses the structure-activity relationships of new fused-ring scaffolds based on imidazopyridine/pyrimidine and furopyridine cores. This library of compounds shows significant potential for anti-trypanosomiases drug discovery. (AU)

FAPESP's process: 17/21146-4 - Heterocyclic chemistry and epigenetic for the development of library of compounds for medicinal chemistry purposes.
Grantee:Flavio da Silva Emery
Support Opportunities: Regular Research Grants
FAPESP's process: 17/22001-0 - Synthesis and evaluation of new heterocyclic compounds as potential antitrypanosomal agents
Grantee:Daniel Gedder Silva
Support Opportunities: Scholarships in Brazil - Post-Doctoral