Effect of 1, 2, 3-triazole salts, non-classical bioisosteres of miltefosine, on Leishmania amazonensis

PHF Stroppa, LMR Antinarelli, AML Carmo… - Bioorganic & Medicinal …, 2017 - Elsevier
Here, we report the effect of new non-classical bioisosteres of miltefosine on Leishmania
amazonensis. Fifteen compounds were synthesized and the compound dhmtAc, containing …

Antileishmanial activity of pyrazolopyridine derivatives and their potential as an adjunct therapy with miltefosine

D Anand, PK Yadav, OPS Patel, N Parmar… - Journal of Medicinal …, 2017 - ACS Publications
A series of pyrazolo (dihydro) pyridines was synthesized and evaluated for antileishmanial
efficacy against experimental visceral leishmaniasis (VL). Among all compounds, 6d and 6j …

Possible Mechanism of Miltefosine-Mediated Death of Leishmania donovani

NK Verma, CS Dey - Antimicrobial agents and chemotherapy, 2004 - Am Soc Microbiol
Miltefosine causes leishmanial death, but the possible mechanism (s) of action is not known.
The mode of action of miltefosine was investigated in vitro in Leishmania donovani …

[HTML][HTML] Miltefosine induces programmed cell death in Leishmania amazonensis promastigotes

FA Marinho, KCS Gonçalves, SS Oliveira… - Memorias do Instituto …, 2011 - SciELO Brasil
In the current study, we evaluated the mechanism of action of miltefosine, which is the first
effective and safe oral treatment for visceral leishmaniasis, in Leishmania amazonensis …

Miltefosine Induces Apoptosis-Like Death in Leishmania donovani Promastigotes

C Paris, PM Loiseau, C Bories… - Antimicrobial agents and …, 2004 - Am Soc Microbiol
ABSTRACT Miltefosine (hexadecylphosphocholine [HePC]) has proved to be a potent oral
treatment for human visceral leishmaniasis due to Leishmania donovani. The molecular …

[HTML][HTML] 1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Leishmania amazonensis Promastigote: An in Vitro Antileishmanial and in …

F Almeida-Souza, VD Silva, GX Silva… - International Journal of …, 2020 - mdpi.com
The current standard treatment for leishmaniasis has remained the same for over 100 years,
despite inducing several adverse effects and increasing cases of resistance. In this study we …

[HTML][HTML] The cytotoxic activity of miltefosine against Leishmania and macrophages is associated with dynamic changes in plasma membrane proteins

KS Fernandes, PEN de Souza, ML Dorta… - Biochimica et Biophysica …, 2017 - Elsevier
In this study, we combined electron paramagnetic resonance (EPR) spectroscopy with an
analysis of biophysical cellular parameters to study the mechanisms underlying the in vitro …

In vitro and in vivo interactions between miltefosine and other antileishmanial drugs

K Seifert, SL Croft - Antimicrobial agents and chemotherapy, 2006 - Am Soc Microbiol
The interaction of miltefosine with amphotericin B, sodium stibogluconate, paromomycin,
and sitamaquine was assessed in vitro and additionally for the first three combinations in …

Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry …

C Borsari, MD Jiménez-Antón, J Eick, E Bifeld… - European Journal of …, 2019 - Elsevier
Leishmaniasis, a major health problem worldwide, has a limited arsenal of drugs for its
control. The appearance of resistance to first-and second-line anti-leishmanial drugs …

Miltefosine resistance in Leishmania donovani involves suppression of oxidative stress-induced programmed cell death

J Mishra, S Singh - Experimental parasitology, 2013 - Elsevier
Abstract Miltefosine (MIL), an alkylphospholipid, is the first orally administrable anti-
leishmanial drug. But due to its long half-life, miltefosine is highly vulnerable for resistance …