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 …
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
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 …
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 …
In continuation of our previous study to identify multitarget inhibitors of cholinesterases
(ChEs) and monoamine oxidase (MAOs) isoforms, we synthesized and evaluated 2 …
(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
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 …
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 …
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
Natural products have significantly contributed to drug discovery for neurodegenerative
diseases. Caffeine is one of the well‐known central nervous system (CNS)‐active natural …
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) …
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 …
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 …
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
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 …
(9a–9l) were designed and synthesized. The potential multi-target profiles of these …