Shital M. Dekate, Kishor M. Hatzade, Ajay M. Ghatole
{"title":"Imidazole–Thiazole Hybrid: Synthesis, Brain Penetration, Cytochrome P450 Enzyme and Gastrointestinal Absorption Study","authors":"Shital M. Dekate, Kishor M. Hatzade, Ajay M. Ghatole","doi":"10.1007/s40995-023-01496-6","DOIUrl":null,"url":null,"abstract":"<div><p>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.</p></div>","PeriodicalId":600,"journal":{"name":"Iranian Journal of Science and Technology, Transactions A: Science","volume":"47 4","pages":"1081 - 1096"},"PeriodicalIF":1.4000,"publicationDate":"2023-07-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Iranian Journal of Science and Technology, Transactions A: Science","FirstCategoryId":"4","ListUrlMain":"https://link.springer.com/article/10.1007/s40995-023-01496-6","RegionNum":4,"RegionCategory":"综合性期刊","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"MULTIDISCIPLINARY SCIENCES","Score":null,"Total":0}
引用次数: 0
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.
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