Results 11 to 20 of about 465 (157)

A Plausible Prebiotic One‐Pot Synthesis of Orotate and Pyruvate Suggestive of Common Protometabolic Pathways

open access: yesAngewandte Chemie, Volume 134, Issue 11, March 7, 2022., 2022
A prebiotic synthesis of the nucleobase orotate, and the citric acid cycle intermediate pyruvate, proceeds in a single pot from two small glycine derivatives, hydantoin and glyoxylate, under mild aqueous conditions. These findings support a co‐evolution of pathways to core protometabolites and nucleic acid building blocks in a common environment ...
Alyssa P. Clay   +5 more
wiley   +2 more sources

Brønsted Base‐Catalyzed Enantioselective α‐Functionalization of Carbonyl Compounds Involving π‐Extended Enolates

open access: yesThe Chemical Record, Volume 23, Issue 11, November 2023., 2023
Efforst are described for developing Brønsted base‐catalyzed, site‐ and stereoselective α‐functionalization of a variety of unsaturated enolizable carbonyl compounds via transient enolates featuring an extended π‐system. Abstract Chiral Brønsted base (BB) catalyzed asymmetric transformations constitute an important tool for synthesis.
Mikel Oiarbide, Claudio Palomo
wiley   +1 more source

Tailored Aza‐Michael Addition as Key Step in the Synthesis of 1H‐imidazo[5,1‐c][1,4]oxazine Scaffolds

open access: yesEuropean Journal of Organic Chemistry, Volume 2022, Issue 40, October 26, 2022., 2022
A new strategy has been proposed for the synthesis of an array of imidazo[5,1‐c][1,4]oxazine chemotypes by using a planned aza‐Michael addition in a 3‐CR heteroring‐forming, post‐cyclization transformation followed by an intramolecular fused‐heterocycles formation process.
Giacomo Mari   +4 more
wiley   +1 more source

A recent update on new synthetic chiral compounds with antileishmanial activity

open access: yesChirality, Volume 34, Issue 10, Page 1279-1297, October 2022., 2022
∎ Abstract Parasitic diseases, including malaria, leishmaniasis, and trypanosomiasis, affect billions of people and are responsible for almost 500,000 deaths/year. In particular, leishmaniasis, a neglected tropical disease, is considered a global public health problem because current drugs have several drawbacks including to toxicity, high cost, and ...
Michele Verboni   +2 more
wiley   +1 more source

Design, synthesis, and characterization of PROTACs targeting the androgen receptor in prostate and lung cancer models

open access: yesArchiv der Pharmazie, Volume 355, Issue 5, May 2022., 2022
Structurally distinct enzalutamide‐based proteolysis‐targeting chimeras (PROTACs) were designed, synthesized, and biochemically analyzed. For the first time, androgen receptor degraders were evaluated in lung cancer cells, where significant degradation of the target was observed.
Lukas M. Gockel   +8 more
wiley   +1 more source

Heterocyclic systems containing S/N regioselective nucleophilic competition: Facile synthesis, antitubercular and antimicrobial activity of thiohydantoins and iminothiazolidinones containing the benzo [PDF]

open access: yesJournal of the Serbian Chemical Society, 2005
The required compounds N-aryl-N'-(3-chloro-2-benzo[b]thenoyl)-thioureas 1a-k were prepared by condensing 3-chloro-2-benzo[b]thenoyl chloride with different arylamines using ammonium thiocyanate, which in turn when treated with chloroacetic acid, yielded ...
Kachhadia V.V., Patel M.R., Joshi H.S.
doaj   +1 more source

Convenient Synthesis of 2-Thioimidazolone/Menadione Conjugates via a Two-Step Sequence Starting with Direct Amination of Menadione

open access: yesSynOpen, 2020
A convenient route to conjugates of 2-thiohydantoins and menadione with linkers of various chemical nature through a two-stage reaction sequence (direct amination of the menadione with a functional amine followed by modification of a functional group) is
Dmitry A. Guk   +3 more
doaj   +1 more source

Synthesis and Biological Evaluation of Novel Dispiro-Indolinones with Anticancer Activity

open access: yesMolecules, 2023
Novel variously substituted thiohydantoin-based dispiro-indolinones were prepared using a regio- and diastereoselective synthetic route from 5-arylidene-2-thiohydantoins, isatines, and sarcosine.
Yan A. Ivanenkov   +10 more
doaj   +1 more source

Synthesis and Fluorescence Mechanism of the Aminoimidazolone Analogues of the Green Fluorescent Protein: Towards Advanced Dyes with Enhanced Stokes Shift, Quantum Yield and Two‐Photon Absorption

open access: yesEuropean Journal of Organic Chemistry, Volume 2021, Issue 41, Page 5649-5660, November 8, 2021., 2021
Intramolecularly hydrogen‐bonded analogues of the green fluorescence protein chromophore with an aminoimidazole moiety were synthesised and characterised. The fluorescence mechanism and substituent effects were investigated in a combined experimental‐computational approach, and a 279‐fold improvement in the quantum yield was realised.
Ervin Kovács   +7 more
wiley   +1 more source

Antidiabetic Potential of Novel 1,3,5-Trisubstituted-2-Thioxoimidazloidin-4-One Analogues: Insights into α-Glucosidase, α-Amylase, and Antioxidant Activities

open access: yesPharmaceuticals, 2022
As the ninth leading cause of death globally, diabetes mellitus (DM) is considered to be the worst chronic metabolic disease requiring an enormous need for healthcare with over 578 million expected cases by 2023. Several recent findings have demonstrated
Salma M. Khirallah   +7 more
doaj   +1 more source

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