Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer’s disease
| Autor: | Rajesh D. Das, Kamala K. Vasu, Nirupa B. Panchal, Sneha R. Sagar, V. Sudarsanam, Manish Nivsarkar, Devendra Singh |
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| Rok vydání: | 2021 |
| Předmět: |
Male
Antioxidant medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science Inflammation Disease Pharmacology medicine.disease_cause 01 natural sciences Biochemistry Neuroprotection Rats Sprague-Dawley Structure-Activity Relationship chemistry.chemical_compound Alzheimer Disease In vivo Formaldehyde Drug Discovery medicine Aluminum Chloride Animals Edema Spectral data Molecular Biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Anti-Inflammatory Agents Non-Steroidal Organic Chemistry Imidazoles Rats 0104 chemical sciences Carrageenan 010404 medicinal & biomolecular chemistry Neuroprotective Agents chemistry Molecular Medicine Female medicine.symptom Oxidative stress |
| Zdroj: | Bioorganic & Medicinal Chemistry. 36:116091 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2021.116091 |
| Popis: | Alzheimer's disease (AD) is a neurodegenerative disease majorly affecting old age populations. Various factors that affect the progression of the disease include, amyloid plaque formation, neurofibrillary tangles, inflammation, oxidative stress, etc. Herein we report of a new series of substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones. The designed compounds were synthesized and characterized by spectral data. In vivo anti-inflammatory activity was carried out for screening of anti-inflammatory potential of synthesized compounds. All the compounds were tested for acute inflammatory activity by using carrageenan induced acute inflammation model. Compounds 10b, 10c, and 10o had shown promising acute anti-inflammatory activity and they were further tested for formalin induced chronic inflammation model. Compound 10c showed both acute and chronic anti-inflammatory activity. Compound 10c also showed promising results in AlCl3 induced AD model. Studies on various behavioral parameters suggested improved amnesic performance of compound 10c treated rats. Compound 10c treated rats also exhibited excellent antioxidant and neuroprotective effect with inherent gastrointestinal safety. |
| Databáze: | OpenAIRE |
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