Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi - SPECIAL ISSUE "NEW TALENT: EUROPE"

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Vahermo , M , Krogerus , S , Nasereddin , A , Kaiser , M , Brun , R , Jaffe , C L , Yli-Kauhaluoma , J & Moreira , V M 2016 , ' Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi - SPECIAL ISSUE "NEW TALENT: EUROPE" ' , MedChemComm , vol. 7 , no. 3 , pp. 457-463 . https://doi.org/10.1039/c5md00498e

Title: Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi - SPECIAL ISSUE "NEW TALENT: EUROPE"
Author: Vahermo, Mikko; Krogerus, Sara; Nasereddin, Abdelmajeed; Kaiser, Marcel; Brun, Reto; Jaffe, Charles L.; Yli-Kauhaluoma, Jari; Moreira, Vânia M.
Contributor: University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
Date: 2016
Language: eng
Number of pages: 7
Belongs to series: MedChemComm
ISSN: 2040-2503
URI: http://hdl.handle.net/10138/224635
Abstract: 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.
Subject: ABIETANE DITERPENOIDS
IN-VITRO
STAPHYLOCOCCUS-AUREUS
TRYPANOCIDAL ACTIVITY
SCREENING DRUGS
DISEASES
CHEMOTHERAPY
AMASTIGOTES
ORGANISMS
1182 Biochemistry, cell and molecular biology
317 Pharmacy
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