一些噻唑基和恶唑基喹唑啉衍生物的合成。

IF 2.5 4区 化学 Q3 CHEMISTRY, ORGANIC
Krishana Kumar Sharma, Gandharve Kumar, Shoma Devi, Gajendra Kumar
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引用次数: 0

摘要

简介:喹唑啉在药物化学中具有重要意义,包括在一系列药物,临床竞争者和生物活性化合物中。喹唑啉类含n杂环化合物具有广泛而独特的生物制药活性。方法:以6-甲基喹唑啉-3(4H)胺和4-取代苯甲醛为起始原料,合成了一系列新合成的杂环化合物N-(4-取代苄基)-2-(2-氨基噻唑-4-基)-6-甲基喹唑啉-3(4H)胺(3a'-3e')和N-(4-取代苄基)-2-(2-氨基恶唑-4-基)-6-甲基喹唑啉-3(4H)胺(3a-3e),并对其抗菌和抗真菌性能进行了评价。并与常用抗菌药物亚胺培南、抗真菌药物咪康唑进行比较。结果:化合物3c′在抑菌活性方面比新合成的其他化合物和标准药物表现出更高的电位活性。结论:通过元素分析和多种光谱技术(1H NMR、13C NMR、IR、GCMS)确定了物质的结构。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of Some Thiazolyl and Oxazolyl Quinazoline Derivatives as Potential Anti-Microbial Agents.

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 (1H NMR, 13C NMR, IR, and GCMS).

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来源期刊
Current organic synthesis
Current organic synthesis 化学-有机化学
CiteScore
3.40
自引率
5.60%
发文量
86
审稿时长
6-12 weeks
期刊介绍: Current Organic Synthesis publishes in-depth reviews, original research articles and letter/short communications on all areas of synthetic organic chemistry i.e. asymmetric synthesis, organometallic chemistry, novel synthetic approaches to complex organic molecules, carbohydrates, polymers, protein chemistry, DNA chemistry, supramolecular chemistry, molecular recognition and new synthetic methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by experts who are internationally known for their eminent research contributions. The journal is essential reading to all synthetic organic chemists. Current Organic Synthesis should prove to be of great interest to synthetic chemists in academia and industry who wish to keep abreast with recent developments in key fields of organic synthesis.
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