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.

ISRN Organic Chemistry Pub Date : 2014-05-06 eCollection Date: 2014-01-01 DOI:10.1155/2014/120173
Thangasamy Elavarasan, Durairaj Peter Bhakiaraj, Mannathusamy Gopalakrishnan
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引用次数: 9

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.

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新型1-(1-芳基- 1h -四唑-5-基)-2-(胡椒苷-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
用胡椒啶在乙腈中分别与2-氯-1-(1-芳基- 1h -四唑-5-基)乙酮(15-21)反应6 h,合成了一系列含四唑核和胡椒啶核的杂环化合物1-(1-芳基- 1h -四唑-5-基)-2-(胡椒啶-1-基)乙酮(22-28)。合成了一系列新的四唑取代哌啶衍生物,并采用串联稀释法对其抑菌活性进行了评价。通过IR、(1)H NMR、(13)C NMR、质谱数据和元素分析对所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,因此可能成为有希望的新先导分子。
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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. A facile stereoselective total synthesis of (R)-rugulactone. Asymmetric organocatalysis at the service of medicinal chemistry. Efficient electrochemical N-alkylation of N-boc-protected 4-aminopyridines: towards new biologically active compounds. Synthesis and biological activities of 4-aminoantipyrine derivatives derived from betti-type reaction.
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