Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in <i>Leishmania infantum</i> Infected Mice

Konstantinović, Jelena; Videnović, Milica; Orsini, Stefania; Bogojević, Katarina; D’Alessandro, Sarah; Scaccabarozzi, Diletta; Jovanović, Nataša Terzić; Gradoni, Luigi; Basilico, Nicoletta; Šolaja, Bogdan A.

doi:10.1021/acsmedchemlett.8b00053

Cited by 10 publications

(12 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Ten out of thirty tested quinoline derivatives that contained adamantine or benzothiophen moiety exhibited IC 50 values less than 1 μM against Leishmania infantum and Leishmania tropica promastigote stage (Konstantinovic et al 2018). Two derivatives, 105 and 106 ( Fig.…”

Section: Antileishmanial Activitymentioning

confidence: 99%

Quinolines and Quinolones as Antibacterial, Antifungal, Anti-virulence, Antiviral and Anti-parasitic Agents

Šenerović

Opsenica

Morić

et al. 2019

Advances in Experimental Medicine and Biology

View full text Add to dashboard Cite

Infective diseases have become health threat of a global proportion due to appearance and spread of microorganisms resistant to majority of therapeutics currently used for their treatment. Therefore, there is a constant need for development of new antimicrobial agents, as well as novel therapeutic strategies. Quinolines and quinolones, isolated from plants, animals, and microorganisms, have demonstrated numerous biological activities such as antimicrobial, insecticidal, antiinflammatory, antiplatelet, and antitumor. For more than two centuries quinoline/quinolone moiety has been used as a scaffold for drug development and even today it represents an inexhaustible inspiration for design and development of novel semi-synthetic or synthetic agents exhibiting broad spectrum of bioactivities. The structural diversity of synthetized compounds provides high and selective activity attained through different mechanisms of action, as well as low toxicity on human cells. This review describes quinoline and quinolone derivatives with antibacterial, antifungal, anti-virulent, antiviral, and anti-parasitic activities with the focus on the last 10 years literature.

show abstract

Section: Antileishmanial Activitymentioning

confidence: 99%

Quinolines and Quinolones as Antibacterial, Antifungal, Anti-virulence, Antiviral and Anti-parasitic Agents

Šenerović

Opsenica

Morić

et al. 2019

Advances in Experimental Medicine and Biology

View full text Add to dashboard Cite

show abstract

“…Moderate‐to‐decent antileishmanial properties are provided by the quinolines tethered to versatile heterocycles at 4‐position through alkyldiamine bridge [40] . One‐third of the evaluated molecules have expressed comparable activity to Amphotericin B (IC 50 =0.13 μM).…”

Section: Antileishmanial Activitymentioning

confidence: 99%

“…Amongst these carbene complexes, one with 2,4,6-trimethoxyphenyl ring appended to imidazolium ring (compound 67, Figure 11 Moderate-to-decent antileishmanial properties are provided by the quinolines tethered to versatile heterocycles at 4position through alkyldiamine bridge. [40] One-third of the Figure 11. Description of the structure of antileishmanial gold-carbene complex.…”

Section: Antileishmanial Activitymentioning

confidence: 99%

See 1 more Smart Citation

Quinoline: A Promising Scaffold in Recent Antiprotozoal Drug Discovery

Dorababu¹

2021

ChemistrySelect

View full text Add to dashboard Cite

Protozoal infections malaria and leishmania have become most prevalent in recent times. A high death rate is reported world‐wide because of these diseases. Although there are only a few antiprotozoal drugs but could not be used anymore to cure protozoal diseases because of their toxic effects. Despite the non‐ceasing attempts to discover the drugs to cure malaria and leishmania, efficient drug‐design with low toxicity could not be achieved. A wide range of heterocyclic pharmacophores have been utilized to design efficient drugs. Amongst these heterocycles, quinoline bicycle is given a high priority, since a vast literature of quinoline derivatives relevant to potent pharmacological properties is available. The efficacy of the drugs lies upon the good bioavailability, favorable pharmacokinetics, and pharmacodynamics of the molecule. In view of these, the continual efforts are being put to bring about potent anti‐protozoal agents to clinical stage. In this review, the potential research done recently towards the anti‐protozoal drug‐design and discovery is compiled comprehensively. The importance of structural features attributed to remarkable activity is described taking consideration of structure‐activity relationship. Safety Index (SI), crucial for clinical efficiency of a drug is compared amongst a set of derivatives which involve inhibitory properties, in addition to the cytotoxic effects.

show abstract

“…For the cytotoxicity assays, cells were seeded in 96-well flat-bottomed (Costar) plates at a concentration of 10 5 cell/mL and incubated at 37°C with 5 % CO 2 . [31] P. Falciparum Cultures and Drug Susceptibility Assay P.f. At the end of the incubation, the MTT method was performed as described in antileishmanial activity section.…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

Novel Hydrophilic Riminophenazines as Potent Antiprotozoal Agents

2019

Self Cite

View full text Add to dashboard Cite

SAR studies on a set of novel hydrophilic C-2 aminopyridinyl riminophenazines bearing variously functionalized basic side chains at C-3 were conducted. The novel compounds were evaluated for in vitro activity against two different species of Leishmania promastigotes, intramacrophage Leishmania amastigotes, chloroquine-sensitive and chloroquine-resistant strains of P. falciparum, and also against mature-stage P. falciparum gametocytes. Their cytotoxicity was evaluated as well on BMDM cell lines. Most of the new compounds potently inhibited the growth of both genera of protozoa with IC 50 values in the high nanomolar range and good selectivities versus mammalian cells. Besides their potent activity against asexual intraerythrocytic stages of P. falciparum, three compounds showed potential as transmission-blocking agents. The key role of the hydrophilic C-2 aminopyridinyl substituent to improve the leishmanicidal activity and the influence of the length and the nature of the basic side chain on the antiprotozoal activity and cytotoxicity were underlined.

show abstract

Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice

Cited by 10 publications

References 21 publications

Quinolines and Quinolones as Antibacterial, Antifungal, Anti-virulence, Antiviral and Anti-parasitic Agents

Quinolines and Quinolones as Antibacterial, Antifungal, Anti-virulence, Antiviral and Anti-parasitic Agents

Quinoline: A Promising Scaffold in Recent Antiprotozoal Drug Discovery

Novel Hydrophilic Riminophenazines as Potent Antiprotozoal Agents

Contact Info

Product

Resources

About