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Synthesis and in Vitro Biological Activity Evaluation of Novel Imidazo [2,1-B][1,3,4] Thiadiazole As Anti-Alzheimer Agents Publisher



Azimi S1 ; Firuzi O2 ; Iraji A2 ; Zonouzi A1 ; Khoshneviszadeh M2 ; Mahdavi M3 ; Edraki N2
Authors
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Authors Affiliations
  1. 1. School of Chemistry, University College of Science, University of Tehran, Tehran, Iran
  2. 2. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
  3. 3. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Source: Letters in Drug Design and Discovery Published:2020


Abstract

Background: Considering that AD is multifactorial in nature, novel series of imidazo [2,1-b][1,3,4] thiadiazole derivatives were designed to address the basic factors responsible for the disease. Methods: These compounds were investigated as inhibitors of beta-site APP cleaving enzyme 1, acetylcholinesterase and butyryl cholinesterase. Results: The BACE1 inhibitory results indicated that nitro phenyl substituted derivatives of imidazo [2,1-b][1,3,4] thiadiazole scaffold (R2 = m-NO2) demonstrated superior BACE1 inhibitory activity compared to other substituted moieties. In the BuChE assay, compounds 4h and 4l carrying meta NO2 at R2 of phenyl ring turned out to be potent inhibitors. Conclusion: In conclusion, these novel synthesized derivatives seem to be promising anti-Alzheimer agents. © 2020 Bentham Science Publishers.
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