ArticleMalaria journal2017
Anti-malarial effect of novel chloroquine derivatives as agents for the treatment of malaria.
Article in Malaria journal, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- Stereoselective design of amino acid bioconjugates: targeting strategies and physicochemical optimization.RSC medicinal chemistry · 2026Review
- Exploring Quinoline Derivatives: Their Antimalarial Efficacy and Structural Features.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Evaluation of the antimalarial activity of SAM13-2HCl with morpholine amide (SKM13 derivative) against antimalarial drug-resistant Plasmodium falciparum and Plasmodium berghei infected ICR mice.Parasites, hosts and diseases · 2024Article
- Dilemma of immunosuppression and infection risk in systemic lupus erythematosus.Rheumatology (Oxford, England) · 2023Article
- In Vitro Evaluation of Two Novel Antimalarial Derivatives of SKM13: SKM13-MeO and SKM13-F.The Korean journal of parasitology · 2022Article
- Anti-malarial activity of HCl salt of SKM13 (SKM13-2HCl).International journal for parasitology. Drugs and drug resistance · 2022Article
- Amino-Acid-Conjugated Natural Compounds: Aims, Designs and Results.Molecules (Basel, Switzerland) · 2022Review
- Article
- Recent Advances in the Discovery of Novel Antiprotozoal Agents.Molecules (Basel, Switzerland) · 2019Review
- Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity.International journal for parasitology. Drugs and drug resistance · 2018Article
Corrections and comments
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe widespread emergence of anti-malarial drug resistance has necessitated the discovery of novel anti-malarial drug candidates. In this study, chloroquine derivatives were evaluated for the improved anti-malarial activity.
resultsNovel two derivatives (SKM13 and SKM14) were synthesized based on the chloroquine (CQ) template containing modified side chains such as α,β-unsaturated amides and phenylmethyl group. The selective index indicated that SKM13 was 1.28-fold more effective than CQ against the CQ-resistant strain Plasmodium falciparum. An in vivo mouse study demonstrated that SKM13 (20 mg/kg) could completely inhibit Plasmodium berghei growth in blood and increased the survival rate from 40 to 100% at 12 days after infection. Haematological parameters [red blood cell (RBC) count, haemoglobin level, and haematocrit level] were observed as an indication of clinical malarial anaemia during an evaluation of the efficacy of SKM13 in a 4-day suppression test. An in vivo study showed a decrease of greater than 70% in the number of RBC in P. berghei-infected mice over 12 days, but the SKM13 (20 mg/kg)-treated group showed no loss of RBC.
conclusionsCQ derivatives with substituents such as α,β-unsaturated amides and phenylmethyl group have enhanced anti-malarial activity against the CQ-resistant strain P. falciparum, and SKM13 is an excellent anti-malarial drug candidate in mice model.
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