A series of fourteen pyrimido[1,2-]benzimidazole compounds was prepared by straightforward heterocyclic chemistry and oxidation methods. The new pyrimidobenzimidazole derivative with a 3-fluorophenyl substituent was identified as a new antiparasitic compound showing excellent activities against parasites. was highly active against promastigotes and amastigotes with EC values in the nanomolar concentration range. Compound was less active than against , but more active against with considerable selectivity. Hence, two promising and selective antiparasitic drug candidates and for the treatment of two parasitic diseases were identified, which can be prepared by green chemistry methods using simple one-pot reactions and oxidation procedures, respectively.
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http://dx.doi.org/10.3390/biomedicines11010219 | DOI Listing |
BMC Res Notes
January 2025
Helen Keller International, New York, USA.
Objective: Sierra Leone, a country where onchocerciasis is endemic in 14 of the 16 districts, was the focus of our investigation. Despite 17 rounds of annual ivermectin treatment since 2005, a report circulated by a local politician indicated an increase in cases of suspected onchocerciasis-related vision impairment in two villages (Mangobo and Petifu) in Tonkolili district. In response, the National Neglected Tropical Disease Program conducted a comprehensive investigation.
View Article and Find Full Text PDFVet Med Sci
January 2025
Department of Zoology, Faculty of Science, Assiut University, Assiut, Egypt.
Background: Fascioliasis represents one of the most significant parasitic and foodborne zoonotic diseases in the world. Resistance to currently deployed human and veterinary flukicides is a growing health problem. Zinc oxide nanoparticles (ZnO-NPs) have developed enormous importance in nanomedicine.
View Article and Find Full Text PDFChem Biodivers
January 2025
University of Lille: Universite de Lille, UMR BioEcoAgro, 3 rue du Professeur Laguesse, 59800, LILLE, FRANCE.
Parasitic diseases such as trypanosomiasis and leishmaniasis pose significant health challenges in Africa. The Senegalese Pharmacopoeia, known for its many medicinal plants with anti-infectious properties, can be a source of antiparasitic natural products. This study aimed to evaluate the in vitro antiparasitic activities of 33 methanolic extracts from 24 ethnopharmacologically selected plants against Trypanosoma brucei brucei and Leishmania mexicana mexicana, as well as their cytotoxic activities on WI-38 cells.
View Article and Find Full Text PDFCrit Rev Oncog
January 2025
School of Pharmaceutical Sciences, Chhatrapati Shahu Ji Maharaj University, Kanpur 208024, India.
This article provides a basic summary of computational research on benzimidazole and its molecular targets in breast cancer (BC) drug discovery. The drug development process is streamlined, expenses are decreased, and the possibility of finding successful therapies for this difficult illness is increased with the use of computational tools. The utilization of benzimidazole derivatives in medication research and discovery is discussed, along with the results of benzimidazole derivative-related clinical trials conducted against blood cancer during the previous five years.
View Article and Find Full Text PDFFront Parasitol
February 2024
Department of Pharmacy Practice and Science, College of Pharmacy, University of Kentucky, Lexington, KY, United States.
An iron-containing milk protein named lactoferrin (Lf) has demonstrated antiparasitic and immunomodulatory properties against a variety of human parasites. This protein has shown its capability to bind and transport iron molecules in the vicinity of the host-pathogen environment. The ability of parasites to sequester the iron molecule and to increase their pathogenicity and survival depends on the availability of iron sources.
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