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Isatin-thiazole hybrids are considered privileged chemical scaffolds due to their broad spectrum of pharmacological properties, making them attractive candidates for drug development. As a result, isatin-thiazole derivatives have emerged as a prominent class of hybrid heterocycles and have been the focus of extensive research in recent years, aiming to address gaps in the discovery of potent new drugs. This review presents a comprehensive survey of the synthetic strategies employed to obtain isatin-thiazole derivatives, highlighting the key reactive sites of the isatin core. In addition, it summarizes the biological activities of isatin-thiazole compounds that exhibit promising anticancer, anticonvulsant, anti-HIV, anti-inflammatory, antidiabetic, and antioxidant properties. The goal of this review is to provide an updated and thorough overview of the synthesis and biological activities for potential applications of isatin-thiazole derivatives, based on studies published up to 2024.
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http://dx.doi.org/10.1002/cbdv.202501989 | DOI Listing |
Chem Biodivers
August 2025
Laboratório De Síntese Orgânica Aplicada, Instituto de Química, Universidade Federal Fluminense, Niterói, Rio de Janeiro, Brazil.
Isatin-thiazole hybrids are considered privileged chemical scaffolds due to their broad spectrum of pharmacological properties, making them attractive candidates for drug development. As a result, isatin-thiazole derivatives have emerged as a prominent class of hybrid heterocycles and have been the focus of extensive research in recent years, aiming to address gaps in the discovery of potent new drugs. This review presents a comprehensive survey of the synthetic strategies employed to obtain isatin-thiazole derivatives, highlighting the key reactive sites of the isatin core.
View Article and Find Full Text PDFBioorg Chem
April 2025
Dr Prabhakar Kore Basic Science Research Centre, KLE Academy of Higher Education and Research, Belagavi 590 010, Karnataka, India.
This study presents the design, synthesis of thiazole-based Hydrazones as potential inhibitors targeting in MDA-MB-231 triple-negative breast cancer cells. A series of quinazoline-thiazole and isatin-thiazole derivatives were synthesized and evaluated for their anti-proliferative activity. Compounds 12d and 12f (quinazoline-thiazole) demonstrated significant inhibitory effects, with IC values of 1.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Pharmacology and Toxicology, KLE College of Pharmacy, Belagavi, KLE Academy of Higher Education and Research, Belagavi 590 010, Karnataka, India.
In the pursuit of novel antidiabetic agents, a series of isatin-thiazole derivatives (7a-7j) were synthesized and characterized using a range of spectroscopic techniques. The enzyme inhibitory activities of the target analogues were assessed using both in vitro and in vivo assays. The tested compounds 7a-7j demonstrated In vitro inhibitory potential against α-glucosidase, as indicated by their IC values ranging from 28.
View Article and Find Full Text PDFCurr Med Chem
June 2024
Laboratory of Planning in Medicinal Chemistry, Department of Pharmaceutical Sciences, Center for Health Sciences, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil.
Background: Cancer is a disease characterized by the abnormal multiplication of cells and is the second leading cause of death in the world. The search for new effective and safe anticancer compounds is ongoing due to factors such as low selectivity, high toxicity, and multidrug resistance. Thus, heterocyclic compounds derived from isatin, thiazole and phthalimide that have achieved promising anticancer activity have been tested in vivo and in clinical trials.
View Article and Find Full Text PDFArch Pharm (Weinheim)
June 2022
Natural and Medical Sciences Research Center, University of Nizwa, Nizwa, Oman.
Diabetes mellitus is one of the most prevalent diseases nowadays. Several marketed drugs are available for the cure and treatment of diabetes, but there is still a dire need of introducing compatible drug molecules with lesser side effects. The current study is based on the synthesis of isatin thiazole derivatives 4-30 via the Hantzsch reaction.
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