Publicación:
The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors
The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors
| dc.contributor.author | Galarreta B.C. | es_PE |
| dc.contributor.author | Sifuentes R. | es_PE |
| dc.contributor.author | Carrillo A.K. | es_PE |
| dc.contributor.author | Sanchez L. | es_PE |
| dc.contributor.author | Amado M.d.R.I. | es_PE |
| dc.contributor.author | Maruenda H. | es_PE |
| dc.date.accessioned | 2024-05-30T23:13:38Z | |
| dc.date.available | 2024-05-30T23:13:38Z | |
| dc.date.issued | 2008 | |
| dc.description | Financial support was received from The Wellcome Trust Travel Awards 2000, 2002; TWAS 02-051; CONCYTEC: 2002-2003, 441-2004 and PUCP-DAI: 3054, 0198, 3414, and E-032. | |
| dc.description.abstract | Twenty-three heterocyclic compounds were evaluated for their potential as trypanothione reductase inhibitors. As a result, the harmaline, 10-thiaisoalloxazine, and aspidospermine frameworks were identified as the basis of inhibitors of Trypanosoma cruzi trypanothione reductase. Two new compounds showed moderately strong, linear competitive inhibition, namely N,N-dimethyl-N-[3-(7-methoxy-1- methyl-3,4-dihydro-9H-b-carbolin-9-yl)propyl]amine (15) and 1,3-bis[3-(dimethylamino)propyl]-1,5- dihydro-2H-pyrimido[4,5-b][1,4]benzothiazine-2,4(3H)-dione (21), with Ki values of 35.1 ± 3.5 lM and 26.9 ±1.9 lM, respectively. Aspidospermine (25) inhibited T. cruzi TryR with a Ki of 64.6 ± 6.2 lM. None of the compounds inhibited glutathione reductase. Their toxicity toward promastigotes of Leishmania amazonensis was assessed. | en |
| dc.description.sponsorship | Consejo Nacional de Ciencia, Tecnología e Innovación Tecnológica - Concytec | |
| dc.identifier.doi | https://doi.org/10.1016/j.bmc.2008.05.074 | |
| dc.identifier.scopus | 2-s2.0-47349130269 | |
| dc.identifier.uri | https://hdl.handle.net/20.500.12390/945 | |
| dc.language.iso | eng | |
| dc.publisher | Elsevier Ltd | en |
| dc.rights | info:eu-repo/semantics/openAccess | |
| dc.subject | Trypanosomatid | en |
| dc.subject | Trypanothione reductase | en |
| dc.subject | Enzymatic inhibition | en |
| dc.title | The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors | |
| dc.type | info:eu-repo/semantics/article | |
| dspace.entity.type | Publication | |
| oairecerif.author.affiliation | #PLACEHOLDER_PARENT_METADATA_VALUE# | |
| oairecerif.author.affiliation | #PLACEHOLDER_PARENT_METADATA_VALUE# | |
| oairecerif.author.affiliation | #PLACEHOLDER_PARENT_METADATA_VALUE# | |
| oairecerif.author.affiliation | #PLACEHOLDER_PARENT_METADATA_VALUE# |