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Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
Sagar, Sneha R; Singh, Devendra Pratap; Das, Rajesh D; Panchal, Nirupa B; Sudarsanam, Vasudevan; Nivsarkar, Manish; Vasu, Kamala K.
Affiliation
  • Sagar SR; Department of Medicinal Chemistry, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India; Institute of Pharmacy, NIRMA University, S. G. Highway, Chandlodia, Gota, Ahmedabad, Gujarat 382481, India.
  • Singh DP; Department of Pharmacology and Toxicology, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India.
  • Das RD; Department of Medicinal Chemistry, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India.
  • Panchal NB; Department of Medicinal Chemistry, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India.
  • Sudarsanam V; Department of Medicinal Chemistry, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India.
  • Nivsarkar M; Department of Pharmacology and Toxicology, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India.
  • Vasu KK; Department of Medicinal Chemistry, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India. Electronic address: kamkva@gmail.com.
Bioorg Med Chem ; 36: 116091, 2021 04 15.
Article in En | MEDLINE | ID: mdl-33676335
ABSTRACT
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Anti-Inflammatory Agents, Non-Steroidal / Neuroprotective Agents / Edema / Alzheimer Disease / Imidazoles / Inflammation Type of study: Prognostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Document type: Article Affiliation country: India

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Anti-Inflammatory Agents, Non-Steroidal / Neuroprotective Agents / Edema / Alzheimer Disease / Imidazoles / Inflammation Type of study: Prognostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Document type: Article Affiliation country: India