Elucidation of the anti-plasmodial activity of novel imidazole and oxazole compounds through computational and experimental approaches.

The development of resistance to conventional antimalarial therapies, along with the unfavorable impact of the COVID-19 pandemic on the global malaria fight, necessitates a greater focus on the search for more effective antimalarial drugs. Targeting a specific enzyme of the malaria parasite to alter its metabolic pathways is a reliable technique for finding antimalarial drug candidates. In this study, we used an technique to test four novel imidazoles and an oxazole derivative for inhibitory potential against Plasmodium lactate dehydrogenase (pLDH), a unique glycolytic enzyme necessary for parasite survival and energy production.

The anti-parasite action of imidazole derivatives likely involves oxidative stress but not HIF-1α signaling.

Background: Therapeutic options for toxoplasmosis are limited. This fact underscores ongoing research efforts to identify and develop better therapy. Previously, we reported the anti-parasitic potential of a new series of derivatives of imidazole.

New imidazoles cause cellular toxicity by impairing redox balance, mitochondrial membrane potential, and modulation of HIF-1α expression.

Background: Our previous reports demonstrated the prospects of a new series of imidazoles as a source of alternative anti-parasite treatments, thus warranting further studies that include toxicity profiling.

Objective: In this study, we evaluated three imidazoles: bis-imidazole (compound 1), phenyl-substituted 1H-imidazole (compound 2), and thiopene-imidazole (compound 3) for cellular toxicity and possible mechanisms.

Methods: The three (3) compounds were assessed for in vitro cytotoxic action.

Imidazole derivatives as antiparasitic agents and use of molecular modeling to investigate the structure-activity relationship.

Toxoplasmosis is a common parasitic disease caused by Toxoplasma gondii. Limitations of available treatments motivate the search for better therapies for toxoplasmosis. In this study, we synthesized a series of new imidazole derivatives: bis-imidazoles (compounds 1-8), phenyl-substituted 1H-imidazoles (compounds 9-19), and thiopene-imidazoles (compounds 20-26).

New Imidazole-Based Compounds Active Against Trypanosoma cruzi.

Background: Current drugs available for the treatment of Chagas disease are fraught with several challenges including severe toxicity and limited efficacy. These factors coupled with the absence of effective drugs for treating the chronic stage of the disease have rendered the development of new drugs against Chagas disease a priority.

Objective: This study screened several imidazole-based compounds for anti-Trypanosoma potential.

Syntheses, structures, and fluorescent properties of 2-(1H-imidazol-2-yl)phenols and their neutral Zn(II) complexes.

A series of 2-(imidazole-2-yl)phenol ligands L1-L6 with the general composition 4-R(4)-5-R(3)-6-R(2)-2-(4,5-R(1),R(1)-1H-imidazole-2-yl)phenol (L1: R(1) = C(2)H(5), R(2) = R(3) = R(4) = H; L2: R(1) = C(6)H(5), R(2) = R(3) = R(4) = H; L3: R(1) = C(6)H(5), R(3) = OCH(3), R(2) = R(4) = H; L4: R(1) = C(6)H(5), R(4) = OCH(3), R(2) = R(3) = H; L5: R(1) = C(6)H(5), R(3) = H, R(2) = R(4) = CH(3); L6: R(1) = C(6)H(5), R(3) = H, R(2) = R(4) = t-Bu) and L7 (2,4-di-tert-butyl-6-(1H-phenanthro[9,10-d]imidazol-2-yl)phenol) and their neutral Zn(II) complexes (Z1-Z7) were synthesized and characterized by spectroscopic and elemental analyses. Molecular structures of L1, L5, Z1, and Z2 were confirmed by single-crystal X-ray diffraction. L1 crystallized in the monoclinic Cc space group, while L5, Z1, and Z2 all crystallized in the triclinic P1 space group.