Synthesis and Antitrypanosomal and Mechanistic Studies of a Series of 2-Arylquinazolin-4-hydrazines: A Hydrazine Moiety as a Selective, Safe, and Specific Pharmacophore to Design Antitrypanosomal Agents Targeting NO Release

Autor: Angel H. Romero, Elena Aguilera, Lourdes Gotopo, Jaime Charris, Noris Rodríguez, Henry Oviedo, Belén Dávila, Gustavo Cabrera, Hugo Cerecetto
Rok vydání: 2022
Předmět:
Zdroj: ACS omega. 7(50)
ISSN: 2470-1343
Popis: Nitric oxide (NO) represents a valuable target to design antitrypanosomal agents by its high toxicity against trypanosomatids and minimal side effects on host macrophages. The progress of NO-donors as antitrypanosomal has been restricted by the high toxicity of their agents, which usually is based on NO-heterocycles and metallic NO-complexes. Herein, we carried out the design of a new class of NO-donors based on the susceptibility of the hydrazine moiety connected to an electron-deficient ring to be reduced to the amine moiety with release of NO. Then, a series of novel 2-arylquinazolin-4-hydrazine, with the potential ability to disrupt the parasite folate metabolism, were synthesized. Their in vitro evaluation against
Databáze: OpenAIRE