Recent Progress in Thiazole, Thiosemicarbazone, and Semicarbazone Derivatives as Antiparasitic Agents Against Trypanosomatids and Plasmodium spp.

Molecules, Год журнала: 2025, Номер 30(8), С. 1788 - 1788

Опубликована: Апрель 16, 2025

Neglected tropical diseases (NTDs), including Chagas disease, human African trypanosomiasis (HAT), leishmaniasis, and malaria, remain a major global health challenge, disproportionately affecting low-income populations. Current therapies for these suffer from significant limitations, such as reduced efficacy, high toxicity, emerging parasite resistance, highlighting the urgent need new therapeutic strategies. In response, substantial efforts have been directed toward synthesis of molecules with improved potency, selectivity, pharmacokinetic profiles. However, despite many compounds exhibiting favorable ADMET (absorption, distribution, metabolism, excretion, toxicity) profiles strong in vitro activity, their translation into vivo models remains limited. Key challenges include lack investment, absence fully representative experimental models, difficulties extrapolating cell-based assay results to more complex biological systems. this review, we analyzed latest advancements (2019–2024) development compound classes, correlating predictive parameters observed activity. Among parameters, highlighted partition coefficient (LogP), which measures compound’s lipophilicity influences its ability cross membranes, Caco-2 cell permeability, an model widely used predict intestinal drug absorption. Additionally, prioritized most promising structural classes pharmaceutical development, discussing structure–activity relationships (SARs) remaining that must be overcome enable clinical application treatment NTDs.

Язык: Английский

Pharmacological Profiles of Neglected Tropical Disease Drugs

Artificial Intelligence in the Life Sciences, Год журнала: 2024, Номер unknown, С. 100116 - 100116

Опубликована: Окт. 1, 2024

Язык: Английский