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

(E-pub Ahead of Print)

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

Journal Name: Letters in Drug Design & Discovery

Become EABM
Become Reviewer


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.

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Ahead of Print)
DOI: 10.2174/1570180816666181108115510
Price: $95