Monoquaternary ammonium derivatives inhibit growth of protozoan parasites

N. Bahamontes-Rosa; A. Robin; A. R. Ambrosio; I. Messias-Reason; E. Beitz; S. L. Flitsch; J. F J Kun

doi:10.1016/j.parint.2007.09.006

Monoquaternary ammonium derivatives inhibit growth of protozoan parasites

N. Bahamontes-Rosa, A. Robin, A. R. Ambrosio, I. Messias-Reason, E. Beitz, S. L. Flitsch, J. F J Kun

Research output: Contribution to journal › Article › peer-review

Abstract

The phospholipid metabolism of Plasmodium falciparum-infected erythrocytes has been shown to be an effective pharmacological target for novel chemotherapy. Thirty-seven monoquaternary ammonium derivatives analogous to choline were screened for their potential antiprotozoal activity against P. falciparum and Leishmania braziliensis. Twenty-three compounds inhibited chloroquine resistant and sensitive P. falciparum strains with inhibitory concentrations ranging from 0.001 μM to 47 μM. Among the inhibitors were six compounds with nanomolar activity containing at least one ethyl group in the polar head and a hydrophobic alkyl chain with 10 to 14 methylene groups. Four compounds also exhibited in vitro antileishmanial properties in the micromolar range. © 2007 Elsevier Ireland Ltd. All rights reserved.

Original language	English
Pages (from-to)	132-137
Number of pages	5
Journal	Parasitology International
Volume	57
Issue number	2
DOIs	https://doi.org/10.1016/j.parint.2007.09.006
Publication status	Published - Jun 2008

Keywords

Aquaporin
Leishmania braziliensis
Monoquaternary ammonium
Phospholipid metabolism
Plasmodium falciparum

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.parint.2007.09.006

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title = "Monoquaternary ammonium derivatives inhibit growth of protozoan parasites",

abstract = "The phospholipid metabolism of Plasmodium falciparum-infected erythrocytes has been shown to be an effective pharmacological target for novel chemotherapy. Thirty-seven monoquaternary ammonium derivatives analogous to choline were screened for their potential antiprotozoal activity against P. falciparum and Leishmania braziliensis. Twenty-three compounds inhibited chloroquine resistant and sensitive P. falciparum strains with inhibitory concentrations ranging from 0.001 μM to 47 μM. Among the inhibitors were six compounds with nanomolar activity containing at least one ethyl group in the polar head and a hydrophobic alkyl chain with 10 to 14 methylene groups. Four compounds also exhibited in vitro antileishmanial properties in the micromolar range. {\textcopyright} 2007 Elsevier Ireland Ltd. All rights reserved.",

keywords = "Aquaporin, Leishmania braziliensis, Monoquaternary ammonium, Phospholipid metabolism, Plasmodium falciparum",

author = "N. Bahamontes-Rosa and A. Robin and Ambrosio, {A. R.} and I. Messias-Reason and E. Beitz and Flitsch, {S. L.} and Kun, {J. F J}",

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TY - JOUR

T1 - Monoquaternary ammonium derivatives inhibit growth of protozoan parasites

AU - Bahamontes-Rosa, N.

AU - Robin, A.

AU - Ambrosio, A. R.

AU - Messias-Reason, I.

AU - Beitz, E.

AU - Flitsch, S. L.

AU - Kun, J. F J

PY - 2008/6

Y1 - 2008/6

N2 - The phospholipid metabolism of Plasmodium falciparum-infected erythrocytes has been shown to be an effective pharmacological target for novel chemotherapy. Thirty-seven monoquaternary ammonium derivatives analogous to choline were screened for their potential antiprotozoal activity against P. falciparum and Leishmania braziliensis. Twenty-three compounds inhibited chloroquine resistant and sensitive P. falciparum strains with inhibitory concentrations ranging from 0.001 μM to 47 μM. Among the inhibitors were six compounds with nanomolar activity containing at least one ethyl group in the polar head and a hydrophobic alkyl chain with 10 to 14 methylene groups. Four compounds also exhibited in vitro antileishmanial properties in the micromolar range. © 2007 Elsevier Ireland Ltd. All rights reserved.

AB - The phospholipid metabolism of Plasmodium falciparum-infected erythrocytes has been shown to be an effective pharmacological target for novel chemotherapy. Thirty-seven monoquaternary ammonium derivatives analogous to choline were screened for their potential antiprotozoal activity against P. falciparum and Leishmania braziliensis. Twenty-three compounds inhibited chloroquine resistant and sensitive P. falciparum strains with inhibitory concentrations ranging from 0.001 μM to 47 μM. Among the inhibitors were six compounds with nanomolar activity containing at least one ethyl group in the polar head and a hydrophobic alkyl chain with 10 to 14 methylene groups. Four compounds also exhibited in vitro antileishmanial properties in the micromolar range. © 2007 Elsevier Ireland Ltd. All rights reserved.

KW - Aquaporin

KW - Leishmania braziliensis

KW - Monoquaternary ammonium

KW - Phospholipid metabolism

KW - Plasmodium falciparum

U2 - 10.1016/j.parint.2007.09.006

DO - 10.1016/j.parint.2007.09.006

M3 - Article

SN - 1383-5769

VL - 57

SP - 132

EP - 137

JO - Parasitology International

JF - Parasitology International

IS - 2

ER -

Monoquaternary ammonium derivatives inhibit growth of protozoan parasites

Abstract

Keywords

UN SDGs

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