GF1061 molecule attacking a Leishmania parasite

A Promising New Weapon Against Leishmaniasis: Fluoroquinoline Derivative

Theo Raines in Health & Wellness December 2025 • 4 min read.

"Scientists explore a novel compound that could revolutionize the treatment of this neglected tropical disease, offering hope for a safer, more effective cure."

Leishmaniasis is a global health challenge, endemic in 98 countries and putting approximately 350 million people at risk. The disease, caused by the Leishmania parasite, manifests in several forms, with visceral leishmaniasis (VL) and cutaneous leishmaniasis (TL) being the most prevalent. Existing treatments have many problems, including toxicity, high cost, and increasing parasite resistance, thus innovations are urgently needed to combat this neglected tropical disease.

Current treatments, which range from pentavalent antimonials to more recent options like miltefosine and liposomal amphotericin B, each present challenges. The older medications can have severe side effects, while newer formulations, though often safer, may be prohibitively expensive for many affected regions. This creates a significant gap in accessible and effective care.

In a recent study, researchers investigated a new fluoroquinoline derivative, 7-chloro-N-(4-fluorophenethyl)quinolin-4-amine (GF1061), for its potential as an antileishmanial agent. Their findings, published in Acta Tropica, reveal the compound's effectiveness against both Leishmania infantum and Leishmania amazonensis species, offering a promising new avenue for treatment development.

GF1061: A Multi-Faceted Attack on Leishmania

GF1061 molecule attacking a Leishmania parasite

The research team rigorously evaluated GF1061 through in vitro and in vivo experiments to understand its antileishmanial properties. They assessed its effectiveness against different Leishmania species, its toxicity to mammalian cells, and its mechanism of action. The results suggest that GF1061 possesses a unique combination of desirable traits.

In laboratory tests, GF1061 demonstrated strong antileishmanial activity against both L. infantum and L. amazonensis. It exhibited high selectivity, meaning it effectively targeted the parasites while showing low toxicity to mammalian cells. The selectivity index (SI) was significantly higher for GF1061 than for amphotericin B (AmpB), a commonly used drug.

Promastigotes: GF1061 showed selectivity indexes of 38.7 and 42.7 against L. infantum and L. amazonensis, respectively.
Amastigotes: GF1061 showed selectivity indexes of 45.0 and 48.9 against L. infantum and L. amazonensis, respectively.
Amphotericin B (AmpB): SI values were significantly lower than GF1061, at 6.6 and 8.8 against promastigotes and 2.2 and 2.7 against amastigotes.

Further investigation revealed that GF1061 disrupts the parasite's mitochondrial function, leading to increased reactive oxygen species (ROS) production and ultimately, cell death by necrosis. This mode of action is particularly attractive, as it circumvents common resistance mechanisms observed with other drugs.

Hope for the Future: GF1061's Potential

The research demonstrates that GF1061 is a promising antileishmanial candidate. Its high efficacy, low toxicity, and novel mechanism of action make it an attractive alternative to current treatments. Furthermore, the successful in vivo results pave the way for further development and eventual clinical trials.

GF1061's effectiveness against Leishmania in infected mice underscores its therapeutic potential. The study revealed significant reductions in parasite load in the infected tissue, liver, spleen, and lymph nodes of treated animals, highlighting its ability to combat the disease in a living system.

While further research is necessary, GF1061 offers renewed hope for individuals affected by leishmaniasis. Its unique properties could lead to the development of a safer, more effective, and more accessible treatment for this devastating disease. With continued investigation, GF1061 may soon transform the landscape of leishmaniasis treatment, offering a brighter future for millions.

About this Article -

This article was crafted using a human-AI hybrid and collaborative approach. AI assisted our team with initial drafting, research insights, identifying key questions, and image generation. Our human editors guided topic selection, defined the angle, structured the content, ensured factual accuracy and relevance, refined the tone, and conducted thorough editing to deliver helpful, high-quality information.See our About page for more information.

This article is based on research published under:

DOI-LINK: 10.1016/j.actatropica.2018.12.036, Alternate LINK

Title: In Vitro And In Vivo Antileishmanial Activity Of A Fluoroquinoline Derivate Against Leishmania Infantum And Leishmania Amazonensis Species

Subject: Infectious Diseases

Journal: Acta Tropica

Publisher: Elsevier BV

Authors: Grasiele S.V. Tavares, Débora V.C. Mendonça, Daniela P. Lage, Luciana M.R. Antinarelli, Tauane G. Soyer, Ana J.S. Senna, Guilherme F. Matos, Daniel S. Dias, Patrícia A.F. Ribeiro, João P.T. Batista, Joana M. Poletto, Geraldo C. Brandão, Miguel A. Chávez-Fumagalli, Guilherme R. Pereira, Elaine S. Coimbra, Eduardo A.F. Coelho

Published: 2019-03-01

Everything You Need To Know

What are the main challenges in treating Leishmaniasis today?

Leishmaniasis is a parasitic disease prevalent in 98 countries, endangering around 350 million people. It's caused by the Leishmania parasite and has different forms, the most common being visceral leishmaniasis (VL) and cutaneous leishmaniasis (TL). Current treatments aren't ideal because of toxicity, high costs, and increasing resistance.

What is 7-chloro-N-(4-fluorophenethyl)quinolin-4-amine (GF1061) and how does it target Leishmania?

The fluoroquinoline derivative, specifically 7-chloro-N-(4-fluorophenethyl)quinolin-4-amine (GF1061), has shown promise in studies. It has demonstrated effectiveness against both *Leishmania infantum* and *Leishmania amazonensis* species. Its mechanism involves disrupting the parasite's mitochondrial function, leading to increased reactive oxygen species (ROS) production and cell death.

How was GF1061 evaluated in the studies?

GF1061 was tested in vitro (in the lab) and in vivo (in animals). Researchers looked at its effectiveness against different Leishmania species, its toxicity to mammalian cells, and how it works. The findings indicate that GF1061 is highly effective against *L. infantum* and *L. amazonensis*, while exhibiting low toxicity to mammalian cells.

How does the selectivity index of GF1061 compare to that of amphotericin B (AmpB)?

GF1061's selectivity index (SI) was notably higher than that of amphotericin B (AmpB), a commonly used drug. For promastigotes, GF1061 showed selectivity indexes of 38.7 and 42.7 against *L. infantum* and *L. amazonensis*, respectively. For amastigotes, the selectivity indexes were 45.0 and 48.9. In contrast, Amphotericin B's SI values were much lower, at 6.6 and 8.8 against promastigotes and 2.2 and 2.7 against amastigotes, showcasing GF1061’s superior targeting of the parasite with less harm to host cells.

Why is GF1061's method of inducing cell death by necrosis considered an advantage in treating Leishmaniasis?

GF1061's ability to induce cell death via necrosis by disrupting mitochondrial function and increasing reactive oxygen species (ROS) is crucial. This mechanism is significant because it can overcome common resistance mechanisms seen with other drugs, which often target different pathways or processes within the parasite. By attacking the mitochondria, a vital organelle for the parasite's survival, GF1061 offers a novel and potentially more durable treatment strategy. Further research is needed to fully understand and optimize this mechanism.