新把戏的老狗:结构不同的5-硝基呋喃和5-亚硝基噻吩亚胺和酰基腙的抗寄生虫潜能

IF 2.3 Q3 PHARMACOLOGY & PHARMACY

Scientia Pharmaceutica Pub Date : 2023-09-19 DOI:10.3390/scipharm91030044

Ibrahim S. Al Nasr, Waleed S. Koko, Tariq A. Khan, Rainer Schobert, Bernhard Biersack

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引用次数: 0

摘要

以5-硝基呋喃醛和5-亚硝基噻吩-2-甲醛为原料制备了杂亚胺和酰基腙。对其抗刚地弓形虫和利什曼原虫活性进行了评价。对某些酰基腙和亚胺具有良好的抗寄生虫作用和选择性。钴(II)和铜(II)配合物保留了3-羟基-2-萘羧基腙的高抗弓形虫活性(2a)。此外，对2a (2b和2i)和吡啶-2-酰基吡唑基亚胺(3g和3h)的各种类似物，观察到对L. major promastigotes的良好活性。对肾细胞和巨噬细胞的毒性相对较低，表明这些化合物具有良好的选择性。

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Old Dogs with New Tricks: Antiparasitic Potential of Structurally Diverse 5-Nitrofuran and 5-Nitrothiophene Imines and Acyl Hydrazones

Miscellaneous imines and acyl hydrazones were prepared from 5-nitrofuraldehyde and 5-nitrothiophene-2-carboxaldehyde. Their activities against Toxoplasma gondii and Leishmania major parasites were evaluated. Promising antiparasitic effects and selectivities were observed for certain acyl hydrazones and imines. Cobalt(II) and copper(II) complexes conserved the high anti-Toxoplasma activities of 3-hydroxy-2-naphthoic carboxyl hydrazone (2a). In addition, sound activities against L. major promastigotes were observed for various analogs of 2a (2b and 2i) and pyrid-2-ylpyrazole-based imines (3g and 3h). Relatively low toxicities to kidney cells and macrophages indicate promising selectivity profiles for these compounds.

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来源期刊

Scientia Pharmaceutica Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

4.60

自引率

4.00%

发文量

审稿时长

10 weeks