Abstract
| Language | English |
|---|---|
| Pages | 457-463 |
| Number of pages | 7 |
| Journal | MedChemComm |
| Volume | 7 |
| Issue number | 3 |
| Early online date | 25 Nov 2015 |
| DOIs | |
| Publication status | Published - 1 Mar 2016 |
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Keywords
- abietane diterpenoids
- in-vitro
- staphylococcus-aureus
- trypanocidal activity
- screening drugs
- diseases
- chemotherapy
- amastigotes
- organisms
Cite this
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Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi. / Vahermo, Mikko; Krogerus, Sara; Nasereddin, Abdelmajeed; Kaiser, Marcel; Brun, Reto; Jaffe, Charles L.; Yli-Kauhaluoma, Jari; Moreira, Vânia M.
In: MedChemComm, Vol. 7, No. 3, 01.03.2016, p. 457-463.Research output: Contribution to journal › Article
TY - JOUR
T1 - Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi
AU - Vahermo, Mikko
AU - Krogerus, Sara
AU - Nasereddin, Abdelmajeed
AU - Kaiser, Marcel
AU - Brun, Reto
AU - Jaffe, Charles L.
AU - Yli-Kauhaluoma, Jari
AU - Moreira, Vânia M.
PY - 2016/3/1
Y1 - 2016/3/1
N2 - Derivatives of dehydroabietic acid bearing different amino acids scaffolds have potent antiprotozoal activity against Leishmania donovani and Trypanosoma cruzi, with good to high selectivity, and can therefore be regarded as good models for further development into new drugs to fight leishmaniasis and Chagas disease. Several of the tested compounds were able to kill parasites residing inside cells, with IC50 values ranging from 2.3 to 9 mu M (L. donovani) and 1.4 to 5.8 mu M (T. cruzi), reflecting their ability to fight these infections at the relevant stage responsible for disease. One of the compounds, bearing a 3-pyridyl-Dalanine side chain, was 1.5-fold more potent against T. cruzi amastigotes residing in L6 cells than the reference compound benznidazole.
AB - Derivatives of dehydroabietic acid bearing different amino acids scaffolds have potent antiprotozoal activity against Leishmania donovani and Trypanosoma cruzi, with good to high selectivity, and can therefore be regarded as good models for further development into new drugs to fight leishmaniasis and Chagas disease. Several of the tested compounds were able to kill parasites residing inside cells, with IC50 values ranging from 2.3 to 9 mu M (L. donovani) and 1.4 to 5.8 mu M (T. cruzi), reflecting their ability to fight these infections at the relevant stage responsible for disease. One of the compounds, bearing a 3-pyridyl-Dalanine side chain, was 1.5-fold more potent against T. cruzi amastigotes residing in L6 cells than the reference compound benznidazole.
KW - abietane diterpenoids
KW - in-vitro
KW - staphylococcus-aureus
KW - trypanocidal activity
KW - screening drugs
KW - diseases
KW - chemotherapy
KW - amastigotes
KW - organisms
UR - http://pubs.rsc.org/en/journals/journalissues/md#!recentarticles&adv
U2 - 10.1039/c5md00498e
DO - 10.1039/c5md00498e
M3 - Article
VL - 7
SP - 457
EP - 463
JO - MedChemComm
T2 - MedChemComm
JF - MedChemComm
SN - 2040-2503
IS - 3
ER -