4.6 Review

The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates

Related references

Note: Only part of the references are listed.
Article Microbiology

Minor Impact of A258D Mutation on Biochemical and Enzymatic Properties of Leishmania infantum GDP-Mannose Pyrophosphorylase

Wei Mao et al.

Summary: Leishmaniasis is a vector-borne disease with limited treatment options. GDP-mannose pyrophosphorylase (GDP-MP) has been identified as a potential therapeutic target for the development of new antileishmanial drugs. In this study, the enzymatic properties of recombinant L. infantum GDP-MP (LiGDP-MP) were analyzed, revealing a mutation at position 258 compared to the homolog in L. donovani. Further studies are needed to determine the significance of this residue change for L. infantum.

MICROORGANISMS (2022)

Review Pharmacology & Pharmacy

Quinoline-based Compounds as Key Candidates to Tackle Drug Discovery Programs of Microbicidal Agents

Aline N. Silva da Gama et al.

Summary: Quinolines are heterocyclic nitrogen compounds widely used as a component in dyes, solvents, pesticides, and have various pharmacological properties such as antimalarial, antiparasitic, antibacterial, antiviral, antifungal, and anticancer activities. A review has been presented on the biological effects and clinical applications of quinolines and their derivatives on three important neglected tropical diseases caused by trypanosomatids, as well as their potential applications towards emerging illnesses caused by fungi, bacteria, and viruses, including the pandemic Covid-19.

CURRENT PHARMACEUTICAL DESIGN (2021)

Article Chemistry, Medicinal

Identification and evaluation of 4-anilinoquin(az)olines as potent inhibitors of both dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV)

Sirle Saul et al.

Summary: This study identified three potent compounds against dengue virus and Venezuelan equine encephalitis virus, all of which showed nearly no toxicity, providing promising prospects for the development of clinical compounds against these emerging viral threats.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2021)

Review Chemistry, Medicinal

Synthetic and medicinal perspective of quinolines as antiviral agents

Ramandeep Kaur et al.

Summary: Quinoline scaffold plays a crucial role in medicinal agents, exhibiting useful biological activities such as anticancer and antibacterial properties. Despite various synthetic strategies developed worldwide, limitations such as side product formation and the use of expensive metal catalysts still exist, prompting ongoing efforts to develop efficient and cost-effective synthetic protocols.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis

Charles E. Mowbray et al.

Summary: A compound with potential therapeutic effects on visceral leishmaniasis has been discovered and optimized to become a potential clinical candidate. This compound has shown strong anti-leishmanial activity in both in vitro and in vivo studies.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Microbiology

Antileishmanial Drug Discovery and Development: Time to Reset the Model?

Ana Isabel Olias-Molero et al.

Summary: Leishmaniasis, caused by Leishmania species, affects humans and animals with no available vaccine and relies mainly on chemotherapy. The currently used drugs are old, toxic, and expensive, with limited efficacy, facing challenges of growing resistance and therapeutic failure. The drug pipeline deconstruction impacts the high failure rate of potential drugs in the fight against this parasitic disease.

MICROORGANISMS (2021)

Article Pharmacology & Pharmacy

Broad spectrum anti-coronavirus activity of a series of anti-malaria quinoline analogues

Leentje Persoons et al.

Summary: This study demonstrated that several quinoline analogues, including chloroquine, hydroxychloroquine, amodiaquine, ferroquine, and mefloquine, exhibit broad-spectrum anti-coronavirus activity in vitro, with chloroquine and hydroxychloroquine showing the most potent effects and favorable selectivity index.

ANTIVIRAL RESEARCH (2021)

Article Health Care Sciences & Services

Safety and Efficacy of Tafenoquine for Plasmodium vivax Malaria Prophylaxis and Radical Cure: Overview and Perspectives

Miles B. Markus

Summary: This article serves as a brief guide on potential adverse events associated with tafenoquine (TQ) intake, summarizing safety and efficacy findings in Plasmodium vivax malaria prophylaxis and radical cure, and highlighting recent TQ-related studies. It also delves into lesser-known biological and other aspects of malaria parasites and 8-aminoquinoline (8-AQ) drug action, while providing explanations on relevant terminology in the field of malaria.

THERAPEUTICS AND CLINICAL RISK MANAGEMENT (2021)

Article Medicine, General & Internal

Estimated Research and Development Investment Needed to Bring a New Medicine to Market, 2009-2018

Olivier J. Wouters et al.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2020)

Article Chemistry, Medicinal

Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines

Sirle Saul et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

Review Pharmacology & Pharmacy

Chloroquine against malaria, cancers and viral diseases

Wenmin Zhou et al.

DRUG DISCOVERY TODAY (2020)

Article Parasitology

Antileishmanial activity of a new chloroquine analog in an animal model of Leishmania panamensis infection

Lizzi Herrera et al.

INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE (2020)

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of new quinoline derivatives as antileishmanial and antitrypanosomal agents

Santiago N. Chanquia et al.

BIOORGANIC CHEMISTRY (2019)

Article Parasitology

Novel benzoxaborole, nitroimidazole and aminopyrazoles with activity against experimental cutaneous leishmaniasis

Katrien Van Bocxlaer et al.

INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE (2019)

Article Medicine, General & Internal

Comparing the Efficacy of Oral Chloroquine versus Oral Tetracycline in the Treatment of Cutaneous Leishmaniasis

Fahmida Malik et al.

JCPSP-JOURNAL OF THE COLLEGE OF PHYSICIANS AND SURGEONS PAKISTAN (2019)

Article Multidisciplinary Sciences

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

Susan Wyllie et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

Article Immunology

GDP-Mannose Pyrophosphorylase: A Biologically Validated Target for Drug Development Against Leishmaniasis

Sebastien Pomel et al.

FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY (2019)

Article Chemistry, Medicinal

Antileishmanial activity of new hybrid tetrahydroquinoline and quinoline derivatives with phosphorus substituents

Ana Tejeria et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents

Akanksha Upadhyay et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study

Julien Pedron et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Physical

Fe3+ chelating quinoline-hydrazone hybrids with proven cytotoxicity, leishmanicidal, and trypanocidal activities

Juan Carlos Coa et al.

PHYSICAL CHEMISTRY CHEMICAL PHYSICS (2018)

Review Microbiology

Recent Development of Visceral Leishmaniasis Treatments: Successes, Pitfalls, and Perspectives

Fabiana Alves et al.

CLINICAL MICROBIOLOGY REVIEWS (2018)

Article Microbiology

Efficacy of Paromomycin-Chloroquine Combination Therapy in Experimental Cutaneous Leishmaniasis

Gert-Jan Wijnant et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2017)

Article Chemistry, Medicinal

Comparative study of structural models of Leishmania donovani and human GDP-mannose pyrophosphorylases

Pierre Daligaux et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Biochemistry & Molecular Biology

Antileishmanial pharmacomodulation in 8-nitroquinolin-2(1H)-one series

Charline Kieffer et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2015)

Article Chemistry, Medicinal

Design, synthesis, ADME characterization and antileishmanial evaluation of novel substituted quinoline analogs

Vadiraj S. Gopinath et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of 2-substituted quinolines as potential antileishmanial agents

Vadiraj S. Gopinath et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Microbiology

Activity of antimalarial drugs in vitro and in a murine model of cutaneous leishmaniasis

Vinicius Pinto Costa Rocha et al.

JOURNAL OF MEDICAL MICROBIOLOGY (2013)

Article Chemistry, Medicinal

Discovery of a new antileishmanial hit in 8-nitroquinoline series

Lucie Paloque et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2012)

Article Microbiology

In Vitro Activities of New 2-Substituted Quinolines against Leishmania donovani

Philippe M. Loiseau et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2011)

Article Microbiology

Increased Glycolytic ATP Synthesis Is Associated with Tafenoquine Resistance in Leishmania major

Jose Ignacio Manzano et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2011)

Article Infectious Diseases

Uptake of the antileishmania drug tafenoquine follows a sterol-dependent diffusion process in Leishmania

Jose Ignacio Manzano et al.

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2011)

Article Microbiology

Antileishmanial and Antitrypanosomal Activities of the 8-Aminoquinoline Tafenoquine

Vanessa Yardley et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2010)

Article Microbiology

Tafenoquine, an Antiplasmodial 8-Aminoquinoline, Targets Leishmania Respiratory Complex III and Induces Apoptosis

Luis Carvalho et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2010)

Review Chemistry, Medicinal

Quinolines and structurally related heterocycles as antimalarials

Kirandeep Kaur et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)

Article Infectious Diseases

Mechanism of interaction of sitamaquine with Leishmania donovani

E. S. Coimbra et al.

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2010)

Article Microbiology

Sitamaquine Sensitivity in Leishmania Species Is Not Mediated by Drug Accumulation in Acidocalcisomes

Carmen Lopez-Martin et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2008)

Article Medicine, Research & Experimental

Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials

Nashira Campos Vieira et al.

BIOMEDICINE & PHARMACOTHERAPY (2008)

Article Medicine, Research & Experimental

Selection and phenotype characterisation of sitamaquine-resistant promastigotes of Leishmania donovani

Christian Bories et al.

BIOMEDICINE & PHARMACOTHERAPY (2008)

Article Medicine, Research & Experimental

Antileishmanial 2-substituted quinolines:: In vitro behaviour towards biological components

Julie Desrivot et al.

BIOMEDICINE & PHARMACOTHERAPY (2007)

Article Biochemical Research Methods

Development of a SPE/HPLC/DAD method for the determination of antileishmanial 2-substituted quinolines and metabolites in rat plasma

Julie Desrivot et al.

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES (2007)

Article Biochemistry & Molecular Biology

Interaction of sitamaquine with membrane lipids of Leishmania donovani promastigotes

Ana Maria Duenas-Romero et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2007)

Review Infectious Diseases

8-aminoquinolines: future role as antiprotozoal drugs

Babu L. Tekwani et al.

CURRENT OPINION IN INFECTIOUS DISEASES (2006)

Article Pharmacology & Pharmacy

In-vitro and in-vivo studies on a topical formulation of sitamaquine dihydrochloride for cutaneous leishmaniasis

Tracy Garnier et al.

JOURNAL OF PHARMACY AND PHARMACOLOGY (2006)

Article Public, Environmental & Occupational Health

A phase II dose-increasing study of sitamaquine for the treatment of visceral leishmaniasis in Kenya

MK Wasunna et al.

AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE (2005)

Article Parasitology

Characterisation of a Leishmania mexicana knockout lacking guanosine diphosphate-mannose pyrophosphorylase

J Stewart et al.

INTERNATIONAL JOURNAL FOR PARASITOLOGY (2005)

Article Chemistry, Medicinal

Biological evaluation of substituted quinolines

X Franck et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2004)

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of substituted quinolines:: Potential treatment of protozoal and retroviral co-infections

MA Fakhfakh et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2003)

Article Chemistry, Medicinal

Substituted quinolines induce inhibition of proliferation of HTLV-1 infected cells

A Fournet et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2003)

Article Chemistry, Organic

Iron-catalysed arylation of heteroaryl halides by Grignard reagents

J Quintin et al.

TETRAHEDRON LETTERS (2002)

Article Public, Environmental & Occupational Health

Phase 2 trial of WR6026, an orally administered 8-aminoquinoline, in the treatment of visceral leishmaniasis caused by Leishmania chagasi

R Dietze et al.

AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE (2001)

Article Chemistry, Organic

Expeditious preparation of 2-substituted quinolines

MA Fakhfakh et al.

TETRAHEDRON LETTERS (2001)

Article Chemistry, Inorganic & Nuclear

Iron catalyzed hydrodebromination of 2-aryl-1,1-dibromo-1-alkenes

MA Fakhfakh et al.

JOURNAL OF ORGANOMETALLIC CHEMISTRY (2001)

Article Chemistry, Medicinal

Synthesis of 2-substituted trifluoromethylquinolines for the evaluation of leishmanicidal activity

J Dade et al.

CHEMICAL & PHARMACEUTICAL BULLETIN (2001)