Synthesis of novel quinazolinone-triheterocyclic hybrides as dual inhibition of urease and ache

IF 2.2 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Journal of the Iranian Chemical Society Pub Date : 2024-08-21 DOI:10.1007/s13738-024-03080-0

Emre Menteşe, Yeter Ünal Güzel, Gülay Akyüz, Nesrin Ünal Karaali

引用次数: 0

Abstract

New triheteroyclic compounds containing quinazolinone, thiophene, andthiadiazole /thiazolidinone structureswere synthesized and characterized by FT-IR, ¹H–NMR, and¹³C–NMRspectral data. The new compounds’ inhibitory activities on urease and acetylcholinesterase were assessed. All triheterocyclic compounds with thiadiazole ring have urease and acetylcholinesteraseinhibitory activities.Especially compound 5a; 3-[(5-(phenylamino)-1,3,4-thiadiazol-2-yl]methyl-2-(thiophen-3-ylmethyl)quinazolin-4(3H)-onehas the best urease inhibition result with 13.30 ± 0.15 µg/mL IC₅₀ value, and it also has the best acetylcholinesterase inhibition with 20.30 ± 0.15 µg/mL IC₅₀ value.

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合成新型喹唑啉酮-三杂环杂化物作为脲酶和胃酸的双重抑制剂

合成了含有喹唑啉酮、噻吩和噻二唑/噻唑烷酮结构的新的三杂环化合物，并通过傅立叶变换红外光谱、1H-NMR 和 13C-NMR 光谱数据对其进行了表征。评估了新化合物对脲酶和乙酰胆碱酯酶的抑制活性。特别是化合物 5a；3-[(5-(苯基氨基)-1,3,4-噻二唑-2-基]甲基-2-(噻吩-3-基甲基)喹唑啉-4(3H)-酮对尿素酶的抑制效果最好，为 13.它对乙酰胆碱酯酶的抑制效果也最好，IC50 值为 20.30 ± 0.15 µg/mL。

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来源期刊

Journal of the Iranian Chemical Society 化学-化学综合

CiteScore

4.40

自引率

8.30%

发文量

230

审稿时长

5.6 months

期刊介绍： JICS is an international journal covering general fields of chemistry. JICS welcomes high quality original papers in English dealing with experimental, theoretical and applied research related to all branches of chemistry. These include the fields of analytical, inorganic, organic and physical chemistry as well as the chemical biology area. Review articles discussing specific areas of chemistry of current chemical or biological importance are also published. JICS ensures visibility of your research results to a worldwide audience in science. You are kindly invited to submit your manuscript to the Editor-in-Chief or Regional Editor. All contributions in the form of original papers or short communications will be peer reviewed and published free of charge after acceptance.