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

Author(s): Sara Azimi, Omidreza Firuzi, Aida Iraji, Afsaneh Zonouzi, Mahsima Khoshneviszadeh, Mohammad Mahdavi*, Najmeh Edraki*.

Journal Name: Letters in Drug Design & Discovery

Volume 17 , Issue 5 , 2020

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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.

Keywords: Alzheimer's disease, BACE1, Imidazo[2, 1-b][1, 3, 4] thiadiazol, AChE, BuChE, synthesize.

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VOLUME: 17
ISSUE: 5
Year: 2020
Page: [610 - 617]
Pages: 8
DOI: 10.2174/1570180816666181108115510
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