Imidazole–Thiazole Hybrid: Synthesis, Brain Penetration, Cytochrome P450 Enzyme and Gastrointestinal Absorption Study

IF 1.4 4区 综合性期刊 Q2 MULTIDISCIPLINARY SCIENCES Iranian Journal of Science and Technology, Transactions A: Science Pub Date : 2023-07-17 DOI:10.1007/s40995-023-01496-6
Shital M. Dekate, Kishor M. Hatzade, Ajay M. Ghatole
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Abstract

Thiazoles, imidazoles, and related derivatives are prominent heterocyclic molecules. Even though the chemistry of imidazole compounds with thiazole moiety has an ancient legacy, the rigorous search for biologically active substances in the imidazole series barely emerged in the last few cascades. The purpose of this communication is to highlight medicinally active substances, while also recent syntheses, which have been reported to still have antimicrobial activities. The present investigation identifies the synthesis and spectroscopic characterization of new 2-amino-4-aryl-1, 3-thiazole-5-carboxaldehydes, their imidazole derivatives, and Schiff bases with various substituted benzaldehydes, including the antimicrobial and antifungal activities among these compounds. The majority of the synthesized compounds are Pgp substrates and CYP3A4 inhibitors, according to the analysis of their pharmacokinetic properties. The overall findings of this study indicated that the molecular to physiologically intriguing imidazole scaffold with varied aromatic substituents was an intriguing methodology for the creation of antibacterial medicines.

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咪唑-噻唑杂合物:合成、脑渗透、细胞色素P450酶及胃肠道吸收研究
噻唑、咪唑及其衍生物是一类重要的杂环分子。尽管含有噻唑基团的咪唑类化合物的化学性质有着悠久的历史,但对咪唑类生物活性物质的严格研究在最近几次级联中几乎没有出现。本通讯的目的是强调药用活性物质,同时也强调最近合成的据报道仍具有抗菌活性的物质。本研究确定了新的2-氨基-4-芳基- 1,3 -噻唑-5-羧醛及其咪唑衍生物和各种取代苯甲醛的希夫碱的合成和光谱表征,包括这些化合物的抗菌和抗真菌活性。根据药代动力学性质分析,合成的化合物大部分为Pgp底物和CYP3A4抑制剂。本研究的总体结果表明,具有不同芳香取代基的分子到生理上有趣的咪唑支架是一种有趣的抗菌药物制造方法。
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来源期刊
CiteScore
4.00
自引率
5.90%
发文量
122
审稿时长
>12 weeks
期刊介绍: The aim of this journal is to foster the growth of scientific research among Iranian scientists and to provide a medium which brings the fruits of their research to the attention of the world’s scientific community. The journal publishes original research findings – which may be theoretical, experimental or both - reviews, techniques, and comments spanning all subjects in the field of basic sciences, including Physics, Chemistry, Mathematics, Statistics, Biology and Earth Sciences
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