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首页> 外文期刊>Future medicinal chemistry >Synthesis, modeling and biological evaluation of hybrids from pyrazolo[1,5c]pyrimidine as antileishmanial agents
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Synthesis, modeling and biological evaluation of hybrids from pyrazolo[1,5c]pyrimidine as antileishmanial agents

机译：吡唑[1,5℃]嘧啶杂交种的合成，建模和生物学评价抗体嗜吡啶

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Aim: A new series of pyrazolo[1,5-c]pyrimidines were synthesized by different hybridization strategies. Methodology: All structures were confirmed by IR, H-1, C-13, H-1-C-13 heteronuclear multiple-quantum correlation (HMQC) spectra and microanalysis. They were evaluated for their in vitro antileishmanial activity against miltefosine and amphotericin B deoxycholate as reference drugs. Results: The most active compounds 2a and 9a demonstrated superior potencies to miltefosine by ten-and six-fold, respectively, for the promastigote form, and by 5.5-fold for the amastigote form. Their binding scenario to Leishmania major pteridine reductase was rationalized by docking experiments. In addition, all compounds were safe for the experimental animals orally up to 150 mg/kg and parenterally up to 75 mg/kg. Conclusion: This study provides novel chemotype class for antileishmanial activity.
机译：目的：通过不同的杂交策略合成新系列的吡唑[1,5-C]嘧啶。 方法论：通过IR，H-1，C-13，H-1-C-13杂核多量子相关（HMQC）光谱和微显分，确认所有结构。 他们评估了对对抗Miltefosine的体外抗碱基活动和两性霉素B脱氧胆酸盐作为参考药物。 结果：最活跃的化合物2A和9A分别向初级蛋白酶分别展示了巨粒素的优异型疗效，用于孕球形式，并为AMASTIGOTE表单进行5.5倍。 通过对接实验合理化它们对Leishmania主要蕨类植物还原酶的结合情景。 此外，所有化合物都是安全的，实验动物口服最高可达150 mg / kg，肠胃外均高达75mg / kg。 结论：本研究为抗恋营养活动提供了新型趋化级。

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