Title : Development of substituted benzylidene derivatives as novel dual cholinesterase inhibitors for Alzheimer's treatment - Gupta_2023_RSC.Adv_13_26344 |
Author(s) : Gupta SM , Behera A , Jain NK , Tripathi A , Rishipathak D , Singh S , Ahemad N , Erol M , Kumar D |
Ref : RSC Adv , 13 :26344 , 2023 |
Abstract :
Leading pathological markers of Alzheimer's disease (AD) include Acetylcholinesterase (AChE), Butyrylcholinesterase (BuChE), Amyloid beta (Abeta) and reactive oxygen species (ROS). Indole derivatives were identified and optimized to improve the potency against AChE, BuChE, Abeta and ROS. The lead molecule IND-30 was found to be selective for AChE (selectivity ratio: 22.92) in comparison to BuChE and showed maximum inhibition potential for human AChE (IC(50): 4.16 +/- 0.063 microM). IND-30 was found to be safe on the SH-SY5Y cell line until the dose of 30 mM. Further, molecule IND-30 was evaluated for its ability to inhibit AChE-induced Abeta aggregation at 0.5, 10 and 20 microM doses. Approximately, 50% of AChE-induced Abeta aggregation was inhibited by IND-30. Thus, IND-30 was found to be multitargeting for AD. |
PubMedSearch : Gupta_2023_RSC.Adv_13_26344 |
PubMedID: 37671344 |
Gupta SM, Behera A, Jain NK, Tripathi A, Rishipathak D, Singh S, Ahemad N, Erol M, Kumar D (2023)
Development of substituted benzylidene derivatives as novel dual cholinesterase inhibitors for Alzheimer's treatment
RSC Adv
13 :26344
Gupta SM, Behera A, Jain NK, Tripathi A, Rishipathak D, Singh S, Ahemad N, Erol M, Kumar D (2023)
RSC Adv
13 :26344