Pyrazol(in)e derivatives of curcumin analogs as a new class of anti- Trypanosoma cruzi agents
| Autor: | Nallely Cabrera, Ruy Pérez-Montfort, Tatiana Saporiti, Christophe Guillon, Marina Sagnou, Guzmán Álvarez, Elena Aguilera, Xavier Robert, Dimitris Matiadis |
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| Přispěvatelé: | National Center for Scientific Research 'Demokritos' (NCSR), Universidad de la República (UDELAR), Universidad de la República [Montevideo] (UCUR), Microbiologie moléculaire et biochimie structurale / Molecular Microbiology and Structural Biochemistry (MMSB), Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Centre National de la Recherche Scientifique (CNRS), Universidad Nacional Autónoma de México (UNAM) |
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Chagas disease
pyrazolines Trypanosoma cruzi [CHIM.THER]Chemical Sciences/Medicinal Chemistry Pharmacology 01 natural sciences 03 medical and health sciences chemistry.chemical_compound Drug Discovery parasitic diseases medicine [SDV.MP.PAR]Life Sciences [q-bio]/Microbiology and Parasitology/Parasitology 030304 developmental biology Biological evaluation 0303 health sciences biology 010405 organic chemistry Chemistry medicine.disease biology.organism_classification 4 5-dihydropyrazoles 0104 chemical sciences 3. Good health Curcumin Molecular Medicine antitrypanosomal agents |
| Zdroj: | Future Medicinal Chemistry Future Medicinal Chemistry, Future Science, 2021, 13 (8), pp.701-714. ⟨10.4155/fmc-2020-0349⟩ |
| ISSN: | 1756-8919 |
| Popis: | Aim: We report the synthesis and biological evaluation of a small library of 15 functionalized 3-styryl-2-pyrazolines and pyrazoles, derived from curcuminoids, as trypanosomicidal agents. Methods & results: The compounds were prepared via a cyclization reaction between the corresponding curcuminoids and the appropriate hydrazines. All of the derivatives synthesized were investigated for their trypanosomicidal activities. Compounds 4a and 4e showed significant activity against epimastigotes of Trypanosoma cruzi, with IC50 values of 5.0 and 4.2 μM, respectively, accompanied by no toxicity to noncancerous mammalian cells. Compound 6b was found to effectively inhibit T. cruzi triosephosphate isomerase. Conclusion: The up to 16-fold higher potency of these derivatives compared with their curcuminoid precursors makes them a promising new family of T. cruzi inhibitors. |
| Databáze: | OpenAIRE |
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