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某些新型1-(1-芳基-1H-四氮唑-5-基)-2-(哌啶-1-基)乙酮衍生物的合成、光谱分析、体外微生物学评价及分子对接研究

Synthesis, Spectral Analysis, In Vitro Microbiological Evaluation, and Molecular Docking Studies of Some Novel 1-(1-Aryl-1H-tetrazol-5-yl)-2-(piperidin-1-yl)ethanone Derivatives.

作者信息

Elavarasan Thangasamy, Bhakiaraj Durairaj Peter, Gopalakrishnan Mannathusamy

机构信息

Synthetic Organic Chemistry Laboratory, Department of Chemistry, Annamalai University, Annamalai Nagar, Tamil Nadu 608 002, India.

出版信息

ISRN Org Chem. 2014 May 6;2014:120173. doi: 10.1155/2014/120173. eCollection 2014.

DOI:10.1155/2014/120173
PMID:24944827
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4040197/
Abstract

A new series of novel heterocyclic compounds containing both tetrazoles and piperidine nuclei together, namely, 1-(1-aryl-1H-tetrazol-5-yl)-2-(piperidin-1-yl)ethanone (22-28), were synthesized by the treatment of the respective 2-chloro-1-(1-aryl-1H-tetrazol-5-yl)ethanone (15-21) with piperidine in acetonitrile for 6 h. A series of novel tetrazole substituted piperidine derivatives were synthesized and evaluated for their antimicrobial activity using serial dilution method. The structures of the synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR, mass spectral data, and elemental analysis. Evaluation of antimicrobial activity shows that several compounds exhibit good activity when compared with the reference drug candidates and thus could be promising new lead molecules.

摘要

通过在乙腈中用哌啶处理相应的2-氯-1-(1-芳基-1H-四唑-5-基)乙酮(15-21)6小时，合成了一系列同时含有四唑和哌啶环的新型杂环化合物，即1-(1-芳基-1H-四唑-5-基)-2-(哌啶-1-基)乙酮(22-28)。合成了一系列新型四唑取代的哌啶衍生物，并采用连续稀释法对其抗菌活性进行了评价。通过红外光谱、(1)H核磁共振、(13)C核磁共振、质谱数据和元素分析对合成化合物的结构进行了表征。抗菌活性评价表明，与参考候选药物相比，几种化合物表现出良好的活性，因此可能是有前途的新先导分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/7e847eb1c3ac/ISRN.ORGANIC.CHEMISTRY2014-120173.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/9d1c6445b6a7/ISRN.ORGANIC.CHEMISTRY2014-120173.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/1d17afd4d645/ISRN.ORGANIC.CHEMISTRY2014-120173.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/404b44ece7ce/ISRN.ORGANIC.CHEMISTRY2014-120173.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/4c35931cd661/ISRN.ORGANIC.CHEMISTRY2014-120173.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/4000a73e0453/ISRN.ORGANIC.CHEMISTRY2014-120173.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/39da208b4d1d/ISRN.ORGANIC.CHEMISTRY2014-120173.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/e7a5b031b7b9/ISRN.ORGANIC.CHEMISTRY2014-120173.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/fc51a259daae/ISRN.ORGANIC.CHEMISTRY2014-120173.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/0c1d9780cdc1/ISRN.ORGANIC.CHEMISTRY2014-120173.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/7e847eb1c3ac/ISRN.ORGANIC.CHEMISTRY2014-120173.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/9d1c6445b6a7/ISRN.ORGANIC.CHEMISTRY2014-120173.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/1d17afd4d645/ISRN.ORGANIC.CHEMISTRY2014-120173.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/404b44ece7ce/ISRN.ORGANIC.CHEMISTRY2014-120173.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/4c35931cd661/ISRN.ORGANIC.CHEMISTRY2014-120173.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/4000a73e0453/ISRN.ORGANIC.CHEMISTRY2014-120173.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/39da208b4d1d/ISRN.ORGANIC.CHEMISTRY2014-120173.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/e7a5b031b7b9/ISRN.ORGANIC.CHEMISTRY2014-120173.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/fc51a259daae/ISRN.ORGANIC.CHEMISTRY2014-120173.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/0c1d9780cdc1/ISRN.ORGANIC.CHEMISTRY2014-120173.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c21d/4040197/7e847eb1c3ac/ISRN.ORGANIC.CHEMISTRY2014-120173.sch.001.jpg

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