一些新的吡唑-嘧啶衍生物的设计、合成、表征及其生物活性评价

Q2 Chemistry Current Chemistry Letters Pub Date : 2023-01-01 DOI:10.5267/j.ccl.2023.2.004
R. Rani, T. Venkatesh, N. Satyanarayan, B. N. Nippu
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引用次数: 0

摘要

本文报道了以取代吡唑醛和巴比妥酸衍生物为原料,以l-脯氨酸为催化剂,通过Knoevengal缩合反应合成了一些新型吡唑-嘧啶衍生物(3a-f)。用光谱方法对合成的化合物进行了结构表征。从抗菌活性来看,与标准药物庆大霉素相比,化合物3d和3f表现出最高的抑制区。细胞毒性实验结果显示,与标准药物阿霉素相比,化合物3e对A549和MCF-7细胞系均具有良好的IC50值。对接研究发现,所有新合成的化合物都与蛋白受体EGFR激酶结构域具有良好的结合能。
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Design, synthesis and characterization of some new pyrazol-pyrimidine derivatives and evaluation of their biological activities
In this work, we have reported a synthesis of some novel pyrazol-pyrimidine derivatives (3a-f) obtained by the reaction of substituted pyrazole aldehydes and barbituric acid derivatives in presence of L-proline as a catalyst via Knoevengal condensation reaction. The structures of the synthesized compounds were characterized by spectral methods. From antibacterial activity, compounds 3d and 3f exhibited highest zone of inhibition as compared to standard drug gentamicin. Cytotoxicity results revealed that compound 3e exhibited a promising IC50 value against both the cell lines (A549 and MCF-7) as compared to the standard drug doxorubicin. Docking study discloses that, all the newly synthesized compounds displayed promising binding energies with the protein receptor EGFR kinase domain.
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来源期刊
Current Chemistry Letters
Current Chemistry Letters Chemistry-Chemistry (all)
CiteScore
4.90
自引率
0.00%
发文量
27
审稿时长
20 weeks
期刊介绍: The "Current Chemistry Letters" is a peer-reviewed international journal which aims to publish all the current and outstanding research articles, reviews and letters in chemistry including analytical chemistry, green chemistry, inorganic chemistry, organic chemistry, physical chemistry, etc. This journal is dedicated to serve all academic and industrial researchers and scientists who are expert in all major advances in chemistry research. The journal aims to provide the most complete and reliable source of information on current developments in these fields. The emphasis will be on publishing quality articles rapidly and openly available to researchers worldwide. Please note readers are free to read, download, copy, distribute, print, search, or link to the full texts of articles published on this journal. Current Chemistry Letters is an open access journal, which provides instant access to the full text of research papers without any need for a subscription to the journal where the papers are published. Therefore, anyone has the opportunity to copy, use, redistribute, transmit/display the work publicly and to distribute derivative works, in any sort of digital form for any responsible purpose, subject to appropriate attribution of authorship. Authors who publish their articles may also maintain the copyright of their articles.
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