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Datusalia, AK and Khatik, GL (2018) Thiazole heterocycle: A privileged scaffold for drug design and discovery. Current Drug Discovery Technologies, 15 (3).

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Abstract

Drug discovery and development is an interesting and challenging topic in current scenario whilst most of the currently available drugs may not be affordable, safe, and therapeutically beneficial due to the development of drug resistance, mutation or exploitation of the existing drugs. Therefore the prime objective for the medicinal chemists is to find out newer efficacious drug or drug like scaffolds to overcome obstacles to meet the current needs. Since heterocyclic compounds are already used as a pool for drug discovery and development viz thiazole, imidazole, tetrazole, flavones, quinolone etc. The thiazole ring is identified as a privileged scaffold which represents a wide range of therapeutic potential such as antidiabetic, antiobesity, anticancer, antimicrobial, CNS activity etc. We have covered various articles which discuss the innovations and research carried out on the thiazole scaffolds in our current thematic issue “Thiazole Heterocycle: A Privileged Scaffold for Drug Design and Discovery”. There are six reviews included from the experts in the field of drug design and synthesis covering the recent updates on the synthesis, pharmacology and applications of thiazole scaffold. G. L. Khatik & colleagues [1] have discussed the important modifications of thiazole ring showing the antidiabetic activity. This includes an extensive review and analysis of thiazole, benzothiazole and thiazolidinones in the development of antidiabetic drugs. Various currently available antidiabetic drugs like rosiglitazone, pioglitazone, troglitazone etc belong to thiazolidinone class of compound that mainly targets the PPAR receptor. Some of the recent target enzymes have also been discussed which have involved in the pathogenesis of diabetes such as alpha-amylase, alpha-glucosidase, SGLT2, dipeptidyl peptidase IV (DPP4) and 11 β -hydroxysteroid dehydrogenase type 1 (11 β -HSD1) where thiazole scaffold serves as the lead compound. D. Sharma & colleagues [2] have discussed the GSK-3β inhibitors based on thiazole moieties. These inhibitors were explored for vast biological activities which include CSNs disorders, cancer and diabetes. The authors highlighted the AstraZeneca molecule ARA014418 based on thiazole ring which was found to be potent GSK-3β inhibitor. A014418 is selective ATP competitive GSK-3β Inhibitor and offers the new arena to develop safer and selective drug. A good compilation of CNS active thiazole derived agents was provided by S. Agarwal & colleague [3], in which they highlighted the use of new leads identification and drug discovery to the CNS targets such as dopamine receptor, adenosine receptor and acetylcholinesterase (AChE). The quest continued to explore thiazoles in the treatment of Alzheimer’s disease, Parkinson’s disease, epilepsy and also as neuroprotective agents. Another significant role of thiazole scaffolds as antimalarial agents was discussed by M.K. Kumawat [4]. The authors envisioned the recent modification in thiazole derivatives which were found to be effective against resistant strain of plasmodium and also explained the SAR in detail.

Item Type: Article
Subjects: Neurodegenerative Disorders
Neuro-Oncological Disorders
Neurocognitive Processes
Neuronal Development and Regeneration
Informatics and Imaging
Genetics and Molecular Biology
Depositing User: Dr. D.D. Lal
Date Deposited: 10 Aug 2018 06:46
Last Modified: 10 Aug 2018 06:46
URI: http://nbrc.sciencecentral.in/id/eprint/428

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