Novel Pyrrole Derivatives as Multi-Target Agents for the Treatment of Alzheimer's Disease: Microwave-Assisted Synthesis, In Silico Studies and Biological Evaluation.

ABSTRACT: Considering the complex pathogenesis of Alzheimer's disease (AD), the multi-target ligand strategy is expected to provide superior effects for the treatment of the neurological disease compared to the classic single target strategy. Thus, one novel pyrrole-based hydrazide (vh0) and four corresponding hydrazide-hydrazones (vh1-4) were synthesized by applying highly efficient MW-assisted synthetic protocols. The synthetic pathway provided excellent yields and reduced reaction times under microwave conditions compared to conventional heating. The biological assays indicated that most of the novel pyrroles are selective MAO-B inhibitors with IC₅₀ in the nanomolar range (665 nM) and moderate AChE inhibitors. The best dual-acting MAO-B/AChE inhibitor (IC₅₀h

SUBMITTER: Mateev E 

PROVIDER: S-EPMC11435393 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature