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一些噻唑基和恶唑基喹唑啉衍生物作为潜在抗菌剂的合成

Synthesis of Some Thiazolyl and Oxazolyl Quinazoline Derivatives as Potential Anti-Microbial Agents.

作者信息

Sharma Krishana Kumar, Kumar Gandharve, Devi Shoma, Kumar Gajendra

机构信息

Department of Pharmacology, Teerthanker Mahaveer College of Pharmacy, Teerthanker Mahaveer University, Moradabad (UP), 244001, India.

Department of Chemistry, FoE, Teerthanker Mahaveer University Moradabad (UP), 244001, India.

出版信息

Curr Org Synth. 2025;22(5):639-648. doi: 10.2174/0115701794320263240918115444.

DOI:10.2174/0115701794320263240918115444
PMID:39844558
Abstract

INTRODUCTION

Quinazoline holds significant importance in pharmaceutical chemistry, which is included in a range of drugs, clinical contenders, and bioactive compounds. N-containing heterocyclic compounds of quinazoline have a wide and distinct range of biopharmaceutical activities.

METHODS

A series of newly synthesized heterocyclic compounds, namely, N-(4-substituted benzylidene)- 2-(2-aminothiazol-4-yl)-6-methylquinazolin-3(4H)-amines (3a'-3e') and N-(4-substituted benzylidene)-2-(2-aminooxazol-4-yl)-6-methylquinazolin-3(4H)-amines (3a-3e), were synthesized starting from 6-methylquinazolin-3(4H)-amine and 4-substituted benzaldehyde and their antibacterial and antifungal properties were evaluated. Moreover, they were compared with the well-known drugs Imipenem (as an antibacterial agent) and Miconazole (as an antifungal).

RESULTS

Compound 3c' exhibited higher potential activity compared to newly synthesized other compounds and standard drugs when tested against the microorganism.

CONCLUSION

The structure of substances was determined through elemental analysis (C.H.N.) and various spectroscopic technique (H NMR, C NMR, IR, and GCMS).

摘要

引言

喹唑啉在药物化学中具有重要意义,它包含在一系列药物、临床候选药物和生物活性化合物中。含氮杂环喹唑啉化合物具有广泛且独特的生物制药活性。

方法

从6-甲基喹唑啉-3(4H)-胺和4-取代苯甲醛出发,合成了一系列新的杂环化合物,即N-(4-取代亚苄基)-2-(2-氨基噻唑-4-基)-6-甲基喹唑啉-3(4H)-胺(3a'-3e')和N-(4-取代亚苄基)-2-(2-氨基恶唑-4-基)-6-甲基喹唑啉-3(4H)-胺(3a-3e),并评估了它们的抗菌和抗真菌性能。此外,还将它们与知名药物亚胺培南(作为抗菌剂)和咪康唑(作为抗真菌剂)进行了比较。

结果

在针对微生物进行测试时,化合物3c'与新合成的其他化合物和标准药物相比,表现出更高的潜在活性。

结论

通过元素分析(C.H.N.)和各种光谱技术(H NMR、C NMR、IR和GCMS)确定了物质的结构。

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