ArticleAntimicrobial agents and chemotherapy2012
Peptidomimetic and organometallic derivatives of primaquine active against Leishmania infantum.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 34 citations in OpenAlex.
- Current developments of metal- and metalloid-based quinoline compounds as leishmanicidal agents.Frontiers in chemistry · 2025Review
- A comprehensive revision on the use of quinoline antimalarial drugs as leishmanicidal agents.Frontiers in chemistry · 2025Review
- Gold(I) and Silver(I) Complexes Containing Hybrid Sulfonamide/Thiourea Ligands as Potential Leishmanicidal Agents.Pharmaceutics · 2024Article
- Article
- Unveiling a New Selenocyanate as a Multitarget Candidate with Anticancer, Antileishmanial and Antibacterial Potential.Molecules (Basel, Switzerland) · 2022Article
- Nanotechnology based solutions for anti-leishmanial impediments: a detailed insight.Journal of nanobiotechnology · 2021Review
- Enhancing the Activity of Drugs by Conjugation to Organometallic Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Review
- Insights into the current status of privileged N-heterocycles as antileishmanial agents.Molecular diversity · 2020Review
- Synthesis and evaluation of novel chromanone and quinolinone analogues of uniflorol as anti-leishmanial agents.Heliyon · 2020Article
- Primaquine derivatives: Modifications of the terminal amino group.European journal of medicinal chemistry · 2019Review
- Chloroquine Analogues as Leads against Pneumocystis Lung Pathogens.Antimicrobial agents and chemotherapy · 2018Article
- Amino Acids in the Development of Prodrugs.Molecules (Basel, Switzerland) · 2018Review
- Article
- N-cinnamoylated aminoquinolines as promising antileishmanial agents.Antimicrobial agents and chemotherapy · 2013Article
- Iron in intracellular infection: to provide or to deprive?Frontiers in cellular and infection microbiology · 2013Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The current treatment of visceral leishmaniasis is made difficult by the low efficacy, elevated costs, low bioavailability, and high toxicity of many of the available drugs. Primaquine, an antimalarial 8-aminoquinoline, displays activity against Leishmania spp., and several of its derivatives have been developed as potential antileishmanial drugs. However, primaquine exhibits low oral bioavailability due to oxidative deamination of its aliphatic chain. We previously developed peptidomimetic and organometallic derivatives of primaquine, with higher resistance to proteolytic degradation and oxidative deamination, which presented significant activity against primaquine-sensitive pathogens such as Plasmodium or Pneumocystis. In light of these relevant findings, we decided to evaluate these compounds against both the promastigote and intramacrophagic amastigote forms of Leishmania infantum, the agent of Mediterranean visceral leishmaniasis. We found that several of these compounds had significant activity against L. infantum. One of the peptidomimetic (3c) and one of the organometallic (7a) derivatives of primaquine were active against the clinically relevant intramacrophagic amastigote form of the parasite, causing >96% reductions in the number of amastigotes per 100 macrophages at 60 and 40 μM, respectively, while being less cytotoxic for host cells than the reference drugs sitamaquine and miltefosine. Hence, compounds 3c and 7a represent new entries toward the development of new antileishmanial leads.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.