Synthesis, biological evaluation and molecular docking study of novel piperidine and piperazine derivatives as multi-targeted agents to treat Alzheimer’s disease

Design, synthesis and evaluation of novel indandione derivatives as multifunctional agents with cholinesterase inhibition, anti-β-amyloid aggregation, antioxidant and neuroprotection properties against Alzheimer’s disease

“…[10][11][12] We are also actively engaged to develop potent MTLDs against AD and recently we have developed piperazine/piperadine and diallyl disulfide analogs as multifunctional agent for the treatment of AD. [13][14] In this report, we have developed a novel series of 1,3 indandione derivatives to study their multifunctional potential against AD. Indandiones and their derivatives are an important class of bioactive molecules which possesses a broad spectrum biological activities such as anticoagulants, anti-microbial, analgesic, anticancer as well as antiviral activity.…”

“…Obtained final products were purified by column chromatography using chloroform and methanol (98:2) as an eluent and fully characterized by 1 HNMR, 13 CNMR, mass spectroscopy as well as elemental analysis. R= …”

“…[13][14] The SH-SY5Y cells were cultured in Dulbecco's minimum essential medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin-streptomycin solution (10,000 units of penicillin and 10 mg of streptomycin in 0.9% NaCl) at 37°C in a humidified atmosphere containing 5% CO 2 . The cells were plated in 96-well plate at a density 2000 cells/well and cultured for 24h.…”

Novel thiazole‐piperazine derivatives as potential cholinesterase inhibitors

“…Two slight less active compounds were 4 and 37 that possessed 3‐methoxyphenyl moiety. The presence of electron‐rich substituents such as hydroxy and methoxy groups on the aromatic ring was identified to support anti‐Alzheimer activity via their antioxidant profile . However, this situation was not observed in compounds 15 and 26 with the 3‐methoxy substituent, whose IC 50 values could not be calculated due to their weak activity.…”

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

“…Hu et al developed a series of 2-methylpiperazine derivatives and evaluated them for CCR5 antagonistic activities based on a calcium mobilization assay. Amongst the synthesized compounds, six compounds (201a-201f) elicited better activity in comparison to the positive control, maraviroc with IC 50 values in the range of 3.0 to 11.7 nm[312].Meena et al have also reported the synthesis and utility of piperazine derivatives in the treatment of Alzheimer's disease[313]. Piplani and Danta synthesized a series of piperazine based hybrid compounds and assessed their cognition enhancing activities through inhibition of .…”