Sharma_2024_RSC.Adv_14_23853

Reference

Title : Unveiling the potential of novel indol-3-yl-phenyl allylidene hydrazine carboximidamide derivatives as AChE\/BACE 1 dual inhibitors: a combined in silico, synthesis and in vitro study - Sharma_2024_RSC.Adv_14_23853
Author(s) : Sharma A , Rudrawar S , Bharate SB , Jadhav HR
Ref : RSC Adv , 14 :23853 , 2024
Abstract :

Considering the failure of many enzyme inhibitors for Alzheimer's disease (AD), research is now focused on multi-target directed drug discovery. In this paper, inhibition of two essential enzymes implicated in AD pathologies, acetylcholinesterase (AChE) and BACE 1 (Beta-site APP Cleaving Enzyme), has been explored. Taking clues from our previous work, 41 novel indol-3-yl phenyl allylidene hydrazine carboximidamide derivatives were synthesized. The results indicated that compounds inhibited both enzymes in micromolar concentrations. Compound 1l is proposed as the most active. In silico, it was seen to occupy the binding pocket of AChE and BACE 1. The ADME predictions showed that these compounds have acceptable physicochemical characteristics. This study provides new leads for the assessment of AChE and BACE 1 dual inhibition as a promising strategy for AD treatment.

PubMedSearch : Sharma_2024_RSC.Adv_14_23853
PubMedID: 39081657

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Citations formats

Sharma A, Rudrawar S, Bharate SB, Jadhav HR (2024)
Unveiling the potential of novel indol-3-yl-phenyl allylidene hydrazine carboximidamide derivatives as AChE\/BACE 1 dual inhibitors: a combined in silico, synthesis and in vitro study
RSC Adv 14 :23853

Sharma A, Rudrawar S, Bharate SB, Jadhav HR (2024)
RSC Adv 14 :23853