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 …
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 …
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 …
Identification of Azelastine and Carvedilol as Cholinesterase Inhibitors via Structure‐Based Virtual Screening of FDA‐approved Drugs
The structure‐based virtual screening (SBVS) has gained immense importance in early drug
discovery. Herein, we report the SBVS‐driven identification of new cholinesterase inhibitors …
discovery. Herein, we report the SBVS‐driven identification of new cholinesterase inhibitors …
Identification of plant-based multitargeted leads for Alzheimer's disease: In-vitro and in-vivo validation of Woodfordia fruticosa (L.) Kurz
Background Alzheimer's disease (AD) is a complex neurodegenerative disease with no
availability of disease-modifying therapeutics. The complex etiology and recent failures in …
availability of disease-modifying therapeutics. The complex etiology and recent failures in …
Multitargeted C9‐substituted ester and ether derivatives of berberrubine for Alzheimer's disease: Design, synthesis, biological evaluation, metabolic stability, and …
R Raghuvanshi, A Jamwal, U Nandi… - Drug Development …, 2023 - Wiley Online Library
Berberrubine is a naturally occurring isoquinoline alkaloid and a bioactive metabolite of
berberine. Berberine exhibits a wide range of pharmacological activities, including …
berberine. Berberine exhibits a wide range of pharmacological activities, including …
A Coumarin− Donepezil Hybrid as a Blood− Brain Barrier Permeable Dual Cholinesterase Inhibitor: Isolation, Synthetic Modifications, and Biological Evaluation of …
Plants have immensely contributed to the drug discovery for neurodegenerative diseases.
Herein, we undertook the phytochemical investigation of Nardostachys jatamansi (D. Don) …
Herein, we undertook the phytochemical investigation of Nardostachys jatamansi (D. Don) …