Fused heterobicyclic systems have gained much importance in the field of medicinal chemistry because of their broad spectrum of physiological activities. Among the heterocyclic rings containing bridgehead nitrogen atom, imidazothiazoles derivatives are especially attractive because of their different biological activities. Since many imidazothiazoles derivatives are effective for treating several diseases, is interesting to analyze the behavior of some isosteric related heterocycles, such as pirrolothiazoles, imidazothiadiazoles and imidazotriazoles. In this context, this review summarizes the current knowledge about the syntheses and biological behavior of these families of heterocycles. Traditional synthetic methodologies as well as alternative synthetic procedures are described. Among these last methodologies, the use of multicomponent reaction, novel and efficient coupling reagents, and environmental friendly strategies, like microwave assistance and solvent-free condition in ionic liquids are also summarized. This review includes the biological assessments, docking research and studies of mechanism of action performed in order to obtain the compounds leading to the development of new drugs.
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http://dx.doi.org/10.1016/j.ejmech.2014.12.012 | DOI Listing |
Chem Biodivers
January 2025
Universite Mohammed Premier Oujda Faculte Pluridisciplinaire de Nador, Department of Chemistry, 60700 Nador, Morocco, Nador, 60700, Nador, MOROCCO.
In recent years, Imidazothiazole-Chalcone conjugates have emerged as notable pharmacophores with potential applications in discovering biologically active compounds. This study focuses on synthesizing novel imidazo[2,1-b]thiazole chalcone derivatives through a facile and conventional process adhering to several principles of green chemistry, facilitating scalable production. The synthesized compounds underwent comprehensive spectroscopic analysis, including 1H NMR, 13C NMR, LC-MS, and FT-IR techniques.
View Article and Find Full Text PDFInflammopharmacology
November 2024
Laboratory of Experimental Cancerology (LabCancer), Department of Biophysics and Physiology, Center for Health Sciences, Federal University of Piauí (UFPI), Universitaria Avenue, Teresina, Piauí, 64049-550, Brazil.
Acute, uncontrolled and/or long-lasting inflammation causes a breakdown in immunological tolerance, leading to chronicity and contributing to a series of significant local or systemic tissue changes. Anti-inflammatory efficacy, fewer adverse effects, improved selectivity, and curative action are imminent issues for patients suffering from chronic inflammation-related pathologies. Then, we performed a complete and critical review about anthelmintics, discussing the main classes and the available preclinical evidence on repurposing to treat inflammation-based conditions.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo, 11829, Egypt. Electronic address:
Breast cancer is the most common invasive cancer diagnosed in women, accounting for most cancer-related fatalities globally. Numerous investigations have revealed that breast cancer is characterized by abnormal expression and maintenance of EGFR levels. In terms of structural study and optimization of several EGFR inhibitors, two series of oxadiazole bearing imidazo[2,1-b]thiazole derivatives were designed and synthesized as potential EGFR inhibitors and assessed for their antitumor activity at NCI-USA.
View Article and Find Full Text PDFParasitol Res
June 2024
Department of Clinical Sciences, College of Medicine, University of Sharjah, Sharjah, 27272, UAE.
Managing primary amoebic meningoencephalitis, induced by Naegleria fowleri poses a complex medical challenge. There is currently no specific anti-amoebic drug that has proven effectiveness against N. fowleri infection.
View Article and Find Full Text PDFSci Rep
April 2024
Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062, India.
A new series of imidazothiazole derivatives bearing thiazolidinone moiety (4a-g and 5a-d) were designed, synthesized and evaluated for potential epidermal growth factor receptor (EGFR) kinase inhibition, anticancer and anti-inflammatory activity, cardiomyopathy toxicity and hepatotoxicity. Compound 4c inhibited EGFR kinase at a concentration of 18.35 ± 1.
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