ReviewMolecular diversity2026
Rational drug design and synthesis of novel bioactive molecules with oxygen heterocycles, including AChE and BChE inhibitory properties and SAR studies.
Review in Molecular diversity, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
1 citing paper in PubMed.
- Recent Developments in Ferulic Acid- and Caffeic Acid-Based Hybrids with Potential Anticancer Properties.Molecules (Basel, Switzerland) · 2026Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
16 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oxygen-containing heterocycles were reviewed as privileged scaffolds that had driven recent advances in rational drug design and synthetic methodology. The manuscript synthesized literature (2015-2025) on oxadiazoles, coumarins, morpholines, pyrans, furans, benzofurans and chromones and summarized how these scaffolds were engineered to optimize potency, selectivity and CNS drug-like properties. Mechanistic analyses demonstrated that oxygen atoms and carbonyl or ether functionalities consistently mediated key hydrogen-bonding and π-interactions within the catalytic anionic site (CAS) and peripheral anionic site (PAS) of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), rationalizing observed AChE/BChE SAR and dual-site binding. Representative medicinal chemistry campaigns were highlighted: coumarin and coumarin-hybrid series provided potent dual-site inhibitors; 1,2-oxadiazoles or 1,3,4-oxadiazoles produced sub to low-nanomolar AChE/BChE leads; morpholine-bearing scaffolds afforded favourable BBB permeability and mixed-type inhibition; and pyranone-carbamate hybrids delivered highly BChE-selective inhibitors with promising in vivo cognitive effects. Synthetic strategies (multicomponent reactions, metal-catalysed cyclizations and green/one-pot protocols) were reviewed and correlated with scaffold diversification and improved ADME profiles. The review concluded by identifying gaps limited unified docking/SAR databases and sparse translational safety data and proposed a workflow combining fragment-based design, dual-site targeting and early ADME profiling to accelerate lead optimisation toward clinically relevant cholinesterase modulators. This focused synthesis of structure activity, mechanism and synthetic access was intended to inform future heterocycle-centric programs against neurodegenerative targets.
Indexed as
Identifiers
41817951What Socratic holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.