Multi-targeting aurones with monoamine oxidase and amyloid-beta inhibitory activities: structure-activity relationship and translating multi-potency to neuroprotection [PDF]
Previously, a series of aurones bearing amine and carbamate functionalities was synthesized and evaluated for their cholinesterase inhibitory activity and drug-like attributes.
Chan, Kit Lam +3 more
core +1 more source
Synthesis of Versatile DNA‐Conjugated Aldehydes by Controlled Oxidation of Amines
A controlled oxidation strategy enables efficient in situ generation of aldehyde‐functionalized DNAs from DNA‐conjugated amines using O2/laccase/TEMPO. This approach facilitates reversible amine–aldehyde transformations for DNA bioconjugation, and provides access to chemically diverse DNA‐encoded libraries, broadening the toolbox for chemical biology ...
Guixian Zhao +6 more
wiley +2 more sources
(E)-3-Heteroarylidenechroman-4-ones as potent and selective monoamine oxidase-B inhibitors [PDF]
A series of (E)-3-heteroarylidenechroman-4-ones (1a-r) was designed, synthesized and investigated in vitro for their ability to inhibit the enzymatic activity of both human monoamine oxidase (hMAO) isoforms, hMAO-A and hMAO-B.
Alcaro, Stefano +6 more
core +1 more source
Biomimetic Pseudopeptides to Decipher the Interplay between Cu and Methionine-Rich Domains in Proteins. [PDF]
Methionine‐rich domains, unity makes strength! Tripodal pseudopeptides mimicking individual binding sites in Met‐rich domains show that the trismethionine environment is highly favorable to stabilize the Cu(I) state. The moderate affinity of a single site is however amplified by efficient statistical and dynamic binding by the many methionine residues.
Badillo-Gómez JI +7 more
europepmc +2 more sources
Assessment of enzyme inhibition : a review with examples from the development of monoamine oxidase and cholinesterase inhibitory drugs [PDF]
Both authors are grateful for the collaborations on multi-target drugs facilitated by COST Action CM1103 (2011-2015).The actions of many drugs involve enzyme inhibition.
Ramsay, Rona R., Tipton, Keith F.
core +1 more source
An integrated approach with new strategies for QSAR models and lead optimization [PDF]
Compound testing set for huAChE collected from Guo et al.
Hui-Hui Hsu +3 more
core +2 more sources
Semicarbazide-sensitive amine oxidase / vascular adhesion protein-1 activity exerts an antidiabetic action in Goto-Kakizaki rats [PDF]
n this study we have explored whether the bifunctional protein semicarbazide-sensitive amine oxidase (SSAO)/vascular adhesion protein-1 (VAP-1) represents a novel target for type 2 diabetes. To this end, Goto-Kakizaki (GK) diabetic rats were treated with
Abella, Anna +11 more
core +1 more source
An innovative iron‐based single‐atom catalyst (FeSA@N‐G) with Fe1–N4 coordination is presented, synthesized through a simple and scalable method. It exhibits exceptional activity and selectivity in N‐alkylation via the borrowing hydrogen strategy under solvent‐free conditions, producing water as the only by‐product. Achieving record TOF (413.1 h-1) and
Arun D. Kute +11 more
wiley +1 more source
Biocatalytic behaviour of immobilized Rhizopus oryzae lipase in the 1,3-selective ethanolysis of sunflower oil to obtain a biofuel similar to biodiesel [PDF]
A new biofuel similar to biodiesel was obtained in the 1,3-selective transesterification reaction of sunflower oil with ethanol using as biocatalyst a Rhizopus oryzae lipase (ROL) immobilized on Sepiolite, an inorganic support.
Bautista, Felipa M. +7 more
core +1 more source
An unusual IRED platform is reported, enabling efficient DKR via reductive amination without any evolutionary engineering. The system accommodates extremely sterically demanding substrates, including naphthyl and quinoline derivatives, delivering naphthyl‐aryl and quinoline‐aryl amine atropisomers with excellent efficiency and stereocontrol (over 80 ...
Zhichao Ni +7 more
wiley +1 more source

