The Current Directions of Searching for Antiparasitic Drugs

Dziduch, Katarzyna; Greniuk, Dominika; Wujec, Monika

doi:10.3390/molecules27051534

Cited by 15 publications

(10 citation statements)

References 79 publications

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“…Additionally, combination approaches involving the use of tamoxifen with meglumine antimoniate and liposomal Amp B with tretazicar have demonstrated promising results [ 62 , 63 ]. Clinical trials have assessed the combined use of AmBisome and miltefosine, revealing encouraging outcomes in immunocompromised patients co-infected with HIV and visceral leishmaniasis [ 64 , 65 ].…”

Section: Resultsmentioning

confidence: 99%

Overview of Research on Leishmaniasis in Africa: Current Status, Diagnosis, Therapeutics, and Recent Advances Using By-Products of the Sargassaceae Family

Abdoul-Latif,

Oumaskour,

Abdallah

et al. 2024

Pharmaceuticals

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Leishmaniasis in Africa, which has been designated as a priority neglected tropical disease by various global organizations, exerts its impact on millions of individuals, primarily concentrated within this particular region of the world. As a result of the progressively grave epidemiological data, numerous governmental sectors and civil organizations have concentrated their endeavors on this widespread outbreak with the objective of devising appropriate remedies. This comprehensive examination delves into multiple facets of this parasitic ailment, scrutinizing the associated perils, diagnostic intricacies, and deficiencies within the existing therapeutic protocols. Despite the established efficacy of current treatments, they are not immune to deleterious incidents, particularly concerning toxicity and the emergence of parasitic resistance, thus accentuating the necessity of exploring alternative avenues. Consequently, this research not only encompasses conventional therapeutic approaches, but also extends its scope to encompass complementary and alternative medicinal techniques, thereby striving to identify innovative solutions. A particularly auspicious dimension of this study lies in the exploration of natural substances and by-products derived from some brown algae of the Sargassaceae family. These resources possess the potential to assume a pivotal role in the management of leishmaniasis.

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Section: Resultsmentioning

confidence: 99%

Overview of Research on Leishmaniasis in Africa: Current Status, Diagnosis, Therapeutics, and Recent Advances Using By-Products of the Sargassaceae Family

Abdoul-Latif,

Oumaskour,

Abdallah

et al. 2024

Pharmaceuticals

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“…Potential antiparasitic drug candidates must not only possess activity against parasites but also not exhibit toxic effects on the host organism [ 28 , 29 ].…”

Section: Resultsmentioning

confidence: 99%

Fused Triazinobenzimidazoles Bearing Heterocyclic Moiety: Synthesis, Structure Investigations, and In Silico and In Vitro Biological Activity

et al. 2023

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[1,3,5]Triazino[1,2-a]benzimidazole-2-amines bearing heterocyclic moiety in 4-position were synthesized. The compounds were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy. The molecular geometry and electron structure of these molecules were theoretically studied using density functional theory (DFT) methods. The molecular structure of the synthesized fused triazinobenzimidazole was confirmed to correspond to the 3,4-dihydrotriazinobenzimidazole structure through the analysis of spectroscopic NMR data and DFT calculations. The antinematodic activity was evaluated in vitro on isolated encapsulated muscle larvae (ML) of Trichinella spiralis. The results showed that the tested triazinobenzimidazoles exhibit significantly higher efficiency than the conventional drug used to treat trichinosis, albendazole, at a concentration of 50 μg/mL. The compound 3c substituted with a thiophen-2-yl moiety exhibited the highest anthelmintic activity, with a larvicidal effect of 58.41% at a concentration of 50 μg/mL after 24 h of incubation. Following closely behind, the pyrrole analog 3f demonstrated 49.90% effectiveness at the same concentration. The preliminary structure-anti-T. spiralis activity relationship (SAR) of the analogues in the series was discussed. The cytotoxicity of the benzimidazole derivatives against two normal fibroblast cells (3T3 and CCL-1) and two cancer human cell lines (MCF-7 breast cancer cells and chronic myeloid leukemia cells AR-230) was evaluated using the MTT-dye reduction assay. The screening results indicated that the compounds showed no cytotoxicity against the tested cell lines. An in silico study of the physicochemical and pharmacokinetic characteristics of the novel synthesized fused triazinobenzimidazoles showed that they were characterized by a significant degree of drug-likeness and optimal properties for anthelmintic agents.

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“…Clofazimine is active against Schistosoma spp for which it reduces the worm burden by >80% [ 29 ]. Further, linezolid and its analogues have antiparasitic activity against the Hymenolepis nana tapeworm [ 30 ]. These agents are part of the second-line agents used in Uganda and were in the TB regimens of >70% our participants.…”

Section: Discussionmentioning

confidence: 99%

Prevalence of Intestinal Helminth Coinfection in Drug-Resistant Tuberculosis in Uganda

Baluku

Nakazibwe

Wasswa

et al. 2022

Open Forum Infectious Diseases

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Background Although a third of people with tuberculosis (TB) are estimated to be co-infected with helminths, the prevalence is largely unknown among people with drug-resistant TB (DRTB). We determined the prevalence of helminth co-infection among people with DRTB in Uganda. Methods In a multi-centre, cross sectional study, eligible Ugandan adults with confirmed DRTB were consecutively enrolled between July to December 2021 at four treatment centres. Socio-demographic data were collected using a questionnaire. Participants underwent anthropometric and blood pressure (BP) measurements, and blood samples were evaluated for random blood glucose (RBG), glycated haemoglobin (HbA1c), non-fasting lipid profile, HIV infection, and a complete blood count. Fresh stool samples were evaluated for adult worms, eggs and larvae using direct microscopy after Kato-Katz concentration techniques. Results Of 212 participants, 156 (73.6%) were male, 118 (55.7%) had HIV and 3 (2.8%) had malaria co-infection. The prevalence of intestinal helminth co-infection was 4.7% (10/212) (95% confidence interval (CI) 2.6–8.6%). The frequency of helminth infections was: Ancylostoma duodenale (n = 4), Schistosoma mansoni (n = 2), Enterobius vermicularis (n = 2), Ascaris lumbricoides (n = 1), and Trichuris trichiuria (n = 1). Conclusion The prevalence of helminth co-infection was low among people with DRTB. More studies are needed to determine the clinical relevance of helminth/DRTB co-infection.

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The Current Directions of Searching for Antiparasitic Drugs

Cited by 15 publications

References 79 publications

Overview of Research on Leishmaniasis in Africa: Current Status, Diagnosis, Therapeutics, and Recent Advances Using By-Products of the Sargassaceae Family

Overview of Research on Leishmaniasis in Africa: Current Status, Diagnosis, Therapeutics, and Recent Advances Using By-Products of the Sargassaceae Family

Fused Triazinobenzimidazoles Bearing Heterocyclic Moiety: Synthesis, Structure Investigations, and In Silico and In Vitro Biological Activity

Prevalence of Intestinal Helminth Coinfection in Drug-Resistant Tuberculosis in Uganda

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