Mechanochemical Synthesis of N-Aryl Amides from O-Protected Hydroxamic Acids.
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DOI: 10.1002/cplu.202000451
Abstract: Two robust and efficient mechanochemical protocols for the synthesis of an array of N-arylamides have been developed. This was achieved by a C-N cross-coupling between O-pivaloyl hydroxamic acids and aryl iodides or aryl boronic acids,… read more here.
Keywords: hydroxamic acids; amides protected; mechanochemical synthesis; aryl amides ... See more keywords
Multifunctional Fe(III)-Binding Polyethers from Hydroxamic Acid-Based Epoxide Monomers.
Sign Up to like & getrecommendations! Published in 2019 at "Macromolecular rapid communications"
DOI: 10.1002/marc.201900282
Abstract: Multiple hydroxamic acids are introduced at poly(ethylene glycol) (PEG) via copolymerization of ethylene oxide with a novel epoxide monomer containing a 1,4,2-dioxazole-protected hydroxamic acid (HAAGE). AB- and ABA-type di- and triblock copolymers as well as… read more here.
Keywords: multifunctional iii; hydroxamic acids; binding polyethers; hydroxamic acid ... See more keywords
Biologically active quinazoline-based hydroxamic acids
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-020-02530-7
Abstract: Molecular hybridization has become a new promising way to treat multifactorial diseases with a single compound that acts on multiple targets. The combination of several functional pharmacophore groups in one molecule can lead to a… read more here.
Keywords: based hydroxamic; quinazoline based; active quinazoline; chemistry ... See more keywords
Exploration of certain 1,3-oxazole- and 1,3-thiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103988
Abstract: Several novel series of hydroxamic acids bearing 2-benzamidooxazole/thiazole (5a-g, 6a-g) or 2-phenylsulfonamidothiazole (8a-c) were designed and synthesized. The compounds were obtained straightforwards via a two step pathway, starting from commercially available ethyl 2-aminooxazole-4-carboxylate or ethyl… read more here.
Keywords: based hydroxamic; inhibitors antitumor; hydroxamic acids; thiazole based ... See more keywords
Exploration of In-silico screening of therapeutic agents against SARS-CoV-2
Sign Up to like & getrecommendations! Published in 2021 at "Chemical Physics"
DOI: 10.1016/j.chemphys.2021.111354
Abstract: In the present investigation, molecular docking studies have been performed using AutoDock Vina to investigate the role of ligand-binding affinity at the hydrophobic pocket of COVID-19. The knowledge of the binding of protein receptors with… read more here.
Keywords: exploration silico; hydroxamic acids; silico screening; sars cov ... See more keywords
Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.06.065
Abstract: A novel series of aniline-containing hydroxamic acids were designed, synthesized and evaluated as anti-virulence agents for the treatment of gastritis and gastric ulcer caused by Helicobacter pylori. In vitro enzyme-based screen together with in vivo assays and… read more here.
Keywords: containing hydroxamic; urease inhibitors; treatment; potent urease ... See more keywords
A safe and selective method for reduction of 2-nitrophenylacetic acid systems to N-aryl hydroxamic acids using continuous flow hydrogenation
Sign Up to like & getrecommendations! Published in 2017 at "Tetrahedron Letters"
DOI: 10.1016/j.tetlet.2017.01.008
Abstract: Abstract The cyclic hydroxamic acid functional group is critical to the biological activity of numerous natural products and drug candidates. Efficient, reliable, and green synthetic methods to produce cyclic hydroxamic acids are needed. Herein, flow… read more here.
Keywords: hydroxamic acids; flow hydrogenation; reduction nitrophenylacetic; nitrophenylacetic acid ... See more keywords
Synthesis of new quinazoline-containing hydroxamic acids as potential HDAC/VEGFR inhibitors. Unusual rearrangements with pyrrolidone ring opening and dehydration of 3-N-hydroxyquinazoline fragment containing tetracycles
Sign Up to like & getrecommendations! Published in 2019 at "Tetrahedron Letters"
DOI: 10.1016/j.tetlet.2019.151315
Abstract: Abstract Synthesis pathways were developed and new hydroxamic acids were obtained as potential inhibitors of HDAC/VEGFR2, including tetracycles containing quinazolinone fragment as a “cap”. Further biological testing of the obtained compounds will give an opportunity… read more here.
Keywords: containing hydroxamic; synthesis new; new quinazoline; hydroxamic acids ... See more keywords
Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01444
Abstract: Hydroxamic acids are outstanding zinc chelating groups that can be used to design potent and selective metalloenzyme inhibitors in various therapeutic areas. Some hydroxamic acids display a high plasma clearance resulting in poor in vivo… read more here.
Keywords: toolbox; plasma stability; chemistry; hydroxamic acids ... See more keywords
Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00232
Abstract: Autotaxin (ATX) catalyzes the hydrolysis of lysophosphatidylcholine (LPC) generating the lipid mediator lysophosphatidic acid (LPA). Both ATX and LPA are involved in various pathological inflammatory conditions, including fibrosis and cancer, and have attracted great interest… read more here.
Keywords: atx; fibrosis; autotaxin; hydroxamic acids ... See more keywords
The Involvement of the Mitochondrial Amidoxime Reducing Component (mARC) in the Reductive Metabolism of Hydroxamic Acids
Sign Up to like & getrecommendations! Published in 2018 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.118.082453
Abstract: The mitochondrial amidoxime reducing component is a recently discovered molybdenum enzyme in mammals which, in concert with the electron transport proteins cytochrome b5 and NADH cytochrome b5 reductase, catalyzes the reduction of N-oxygenated structures. This… read more here.
Keywords: mitochondrial amidoxime; amidoxime reducing; system; metabolism ... See more keywords