Design, synthesis, and pharmacological evaluation of embelin–aryl/alkyl amine hybrids as orally bioavailable blood–brain barrier permeable multitargeted agents with …

VK Nuthakki, S Choudhary, CN Reddy… - ACS chemical …, 2023 - ACS Publications
The complex and multifaceted nature of Alzheimer's disease has brought about a pressing
demand to develop ligands targeting multiple pathways to combat its outrageous …

[HTML][HTML] Recent developments in the design and synthesis of benzylpyridinium salts: Mimicking donepezil hydrochloride in the treatment of Alzheimer's disease

S Sepehri, M Saeedi, B Larijani, M Mahdavi - Frontiers in Chemistry, 2022 - frontiersin.org
Background: Alzheimer's disease (AD) is an advanced and irreversible degenerative
disease of the brain, recognized as the key reason for dementia among elderly people. The …

Design, synthesis, and bioevaluation of indole core containing 2-arylidine derivatives of thiazolopyrimidine as multitarget inhibitors of cholinesterases and monoamine …

M Shahid Nadeem, J Azam Khan, I Kazmi… - ACS omega, 2022 - ACS Publications
In continuation of our previous study to identify multitarget inhibitors of cholinesterases
(ChEs) and monoamine oxidase (MAOs) isoforms, we synthesized and evaluated 2 …

Discovery of blood-brain barrier permeable and orally bioavailable caffeine-based amide derivatives as acetylcholinesterase inhibitors

M Sharma, A Sharma, S Thakur, VK Nuthakki… - Bioorganic …, 2023 - Elsevier
Caffeine is one of the privileged natural products that shows numerous effects on the central
nervous system. Herein, thirty-one caffeine-based amide derivatives were synthesized and …

Synthesis and Biological Evaluation of Colchicine─ Aryl/Alkyl Amine Hybrids as Potential Noncytotoxic Cholinesterase Inhibitors: Identification of SBN-284 as a Dual …

CN Reddy, VK Nuthakki, A Sharma… - ACS Chemical …, 2024 - ACS Publications
Colchicine, one of the oldest anti-inflammatory natural products still used clinically, inhibits
NF-κB signaling and NLRP3 inflammasome activation. Despite its cytotoxicity and narrow …

Design, synthesis, and structure–activity relationship of caffeine‐based triazoles as dual AChE and BACE‐1 inhibitors

M Sharma, A Sharma, VK Nuthakki… - Drug Development …, 2022 - Wiley Online Library
Natural products have significantly contributed to drug discovery for neurodegenerative
diseases. Caffeine is one of the well‐known central nervous system (CNS)‐active natural …

Interest of novel N-alkylpyridinium-indolizine hybrids in the field of Alzheimer's disease: Synthesis, characterization and evaluation of antioxidant activity …

I Baussanne, O Firstova, AB Dediu, C Larosa… - Bioorganic …, 2021 - Elsevier
A small library of molecules combining indolizine and N-alkyl pyridinium was synthesized
and evaluated in a multi-target-directed-ligand strategy for Alzheimer's disease (AD) …

N‐Benzyl piperidine Fragment in Drug Discovery

A Sharma, M Sharma, SB Bharate - ChemMedChem, 2024 - Wiley Online Library
The N‐benzyl piperidine (N‐BP) structural motif is commonly employed in drug discovery
due to its structural flexibility and three‐dimensional nature. Medicinal chemists frequently …

Synthesis and biological evaluation of coumarin triazoles as dual inhibitors of cholinesterases and β-secretase

A Sharma, SB Bharate - ACS omega, 2023 - ACS Publications
Coumarin is a naturally occurring bioactive pharmacophore with wide occurrence among
central nervous system (CNS)-active small molecules. 8-Acetylcoumarin, one of the natural …

Synthesis and biological evaluation of benzimidazoles/1, 3, 5-triazine-2, 4-diamine hybrid compounds: a new class of multifunctional alzheimer targeting agents

S Karimian, M Shekouhy, S Pirhadi, A Iraji… - New Journal of …, 2022 - pubs.rsc.org
In this study, a series of new benzimidazole/1, 3, 5-triazine-2, 4-diamine hybrid derivatives
(9a–9l) were designed and synthesized. The potential multi-target profiles of these …