Caffeine and Purine Derivatives: A Comprehensive Review on the Chemistry, Biosynthetic Pathways, Synthesis‐Related Reactions, Biomedical Prospectives and …

AA Abu‐Hashem, O Hakami, M El‐Shazly… - Chemistry & …, 2024 - Wiley Online Library
Caffeine and purine derivatives represent interesting chemical moieties, which show various
biological activities. Caffeine is an alkaloid that belongs to the family of methylxanthine …

Theophylline-based hybrids as acetylcholinesterase inhibitors endowed with anti-inflammatory activity: synthesis, bioevaluation, in silico and preliminary kinetic …

AA Elgazar, RA El-Domany, WM Eldehna, FA Badria - RSC advances, 2023 - pubs.rsc.org
In this study, we investigated the conjugation of theophylline with different compounds of
natural origin hoping to construct new hybrids with dual activity against cholinergic and …

Recent advances in the natural product analogues for the treatment of neurodegenerative diseases

J Zhang, P Jiang, S Wang, M Li, Z Hao, W Guan… - Bioorganic …, 2024 - Elsevier
Neurodegenerative diseases (NDs) represent a hallmark of numerous incapacitating and
untreatable conditions, the incidence of which is escalating swiftly, exemplified by …

New Benzamides as Multi-Targeted Compounds: A Study on Synthesis, AChE and BACE1 Inhibitory Activity and Molecular Docking

D Drozdowska, D Maliszewski, A Wróbel… - International Journal of …, 2023 - mdpi.com
The synthesis of eleven new and previously undescribed benzamides was designed. These
compounds were specifically projected as potential inhibitors of the enzymes …

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 …

Orally bioavailable styryl derivative of rohitukine-N-oxide inhibits CDK9/T1 and the growth of pancreatic cancer cells

D Bhurta, MM Hossain, M Bhardwaj, F Showket… - European Journal of …, 2023 - Elsevier
The chromone alkaloid is one of the classical pharmacophores for cyclin-dependent kinases
(CDKs) and represents the first CDK inhibitor to reach clinical trials. Rohitukine (1), a …

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 …

Identification of Azelastine and Carvedilol as Cholinesterase Inhibitors via Structure‐Based Virtual Screening of FDA‐approved Drugs

M Sharma, S Thakur, HR Jadhav… - ChemistrySelect, 2023 - Wiley Online Library
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 …

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 …

New Multitarget Molecules Derived from Caffeine as Potentiators of the Cholinergic System

JP Munafó, B Biscussi, D Obiol… - ACS Chemical …, 2024 - ACS Publications
Cholinergic deficit is a characteristic factor of several pathologies, such as myasthenia
gravis, some types of congenital myasthenic syndromes, and Alzheimer's Disease. Two …