First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies

被引：4

作者：

Martin-Montes, Alvaro ^{[1
]}

Jimenez-Falcao, Sandra ^{[2
]}

Gomez-Ruiz, Santiago ^{[3
]}

Marin, Clotilde ^{[1
]}

Mendez-Arriaga, Jose M. ^{[3
]}

机构：

[1] Univ Granada, Dept Parasitol, Ave Fuentenueva, Granada 18071, Spain

[2] Univ Politecn Madrid, Dept Mat & Prod Aerosp ETSI Aeronaut & Espacio, Organ Nanotechnol Lab, Madrid 28040, Spain

[3] Univ Rey Juan Carlos, Dept Biol & Geol Fis & Quim Inorgan, COMET NANO Grp, ESCET, Calle Tulipan S-N, Mostoles 28933, Spain

来源：

PHARMACEUTICALS | 2023年 / 16卷 / 10期

关键词：

metal complex; coordination chemistry; leishmaniasis; antiparasitic activity; drug release; nanoparticles; IN-VITRO; CUTANEOUS LEISHMANIASIS; CHAGAS-DISEASE; TRYPANOSOMA-CRUZI; MESOPOROUS SILICA; TROPICAL DISEASE; CU(II); CHEMOTHERAPY; COPPER(II); DERIVATIVES;

D O I：

10.3390/ph16101380

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Leishmaniasis and Chagas disease are still considered neglected illnesses due to the lack of investment in research, despite the fact that almost one million new cases are reported every year. Four 7-oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine (HftpO) first-row transition complexes (Cu, Co, Ni, Zn) have been studied for the first time in vitro against five different species of Leishmania spp. (L. infantum, L. braziliensis, L. donovani, L. peruviana and L. mexicana) as well as Trypanosoma cruzi, showing higher efficacy than the reference commercial drugs. UV and luminescence properties were also evaluated. As a proof of concept, anchoring of a model high-effective-metal complex as an antiparasitic agent on silica nanoparticles was carried out for the first time, and drug-release behaviour was evaluated, assessing this new approach for drug vehiculation.

引用

页数：19

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