Results 21 to 30 of about 1,063 (182)

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

SynOpen, 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, Olga O. Krasnovskaya, Nikolai V. Zyk, Elena K. Beloglazkina   +3 more
doaj   +1 more source

Synthesis and Identification of Heterobivalent Anticancer Compounds Containing Urea and 5-Arylidene-2-Thiohydantoin Motifs. [PDF]

ChemistrySelect
A synthetic approach to the synthesis of novel heterobivalent compounds containing urea and 5‐arylthiohydantoin groups was developed for the preparation of a mixture‐based library. Through the screening and deconvolution of the library, six hits with βC branched residues at R1 and imidazyl residue at R3 were identified exhibiting moderate inhibitory ...
Whitely C, Winburn H, Li Y.
europepmc   +2 more sources

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

European 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, Levente Cseri, Attila Jancsó, Ferenc Terényi, Anna Fülöp, Balázs Rózsa, Gábor Galbács, Zoltán Mucsi   +7 more
wiley   +1 more source

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

Molecules, 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, Maxim E. Kukushkin, Anastasia A. Beloglazkina, Radik R. Shafikov, Alexander A. Barashkin, Andrey A. Ayginin, Marina S. Serebryakova, Alexander G. Majouga, Dmitry A. Skvortsov, Viktor A. Tafeenko, Elena K. Beloglazkina   +10 more
doaj   +1 more source

Synthesis and Biological Evaluation of Dantrolene‐Like Hydrazide and Hydrazone Analogues as Multitarget Agents for Neurodegenerative Diseases

ChemMedChem, Volume 16, Issue 18, Page 2807-2816, September 16, 2021., 2021
Simpler is better: Structural modifications of the chemical structure of dantrolene, previously disclosed as a repositionable drug with potential for Alzheimer's disease, allowed preparing new small molecules with multitarget activity profile. Compared to dantrolene, molecular simplification resulted in less toxic and more soluble compounds.
Isabella Bolognino, Nicola Giangregorio, Annamaria Tonazzi, Antón L. Martínez, Cosimo D. Altomare, María I. Loza, Sara Sablone, Saverio Cellamare, Marco Catto   +8 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

Pharmaceuticals, 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, Heba M. M. Ramadan, Hossam Aladl Aladl Aladl, Najla O. Ayaz, Lina A. F. Kurdi, Mariusz Jaremko, Samar Zuhair Alshawwa, Essa M. Saied   +7 more
doaj   +1 more source

Protein Adductomics: Methodologies for Untargeted Screening of Adducts to Serum Albumin and Hemoglobin in Human Blood Samples. [PDF]

, 2019
The reaction products of electrophiles in vivo can be measured as adducts to the abundant proteins, hemoglobin (Hb), and human serum albumin (HSA), in human blood samples.
Carlsson, Henrik, Rappaport, Stephen, Törnqvist, Margareta   +2 more
core   +2 more sources

Stapled ACE2 peptidomimetics designed to target the SARS‐CoV‐2 spike protein do not prevent virus internalization

Peptide Science, Volume 113, Issue 4, July 2021., 2021
Abstract COVID‐19 is caused by a novel coronavirus called severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2). Virus cell entry is mediated through a protein‐protein interaction (PPI) between the SARS‐CoV‐2 spike protein and angiotensin‐converting enzyme 2 (ACE2).
Danielle C. Morgan, Caroline Morris, Amit Mahindra, Connor M. Blair, Gonzalo Tejeda, Imogen Herbert, Matthew L. Turnbull, Gauthier Lieber, Brian J. Willett, Nicola Logan, Brian Smith, Andrew B. Tobin, David Bhella, George Baillie, Andrew G. Jamieson   +14 more
wiley   +1 more source

1H-Imidazol-4(5H)-ones and thiazol-4(5H)-ones as emerging pronucleophiles in asymmetric catalysis [PDF]

, 2016
Asymmetric catalysis represents a very powerful tool for the synthesis of enantiopure compounds. In this context the main focus has been directed not only to the search for new efficient chiral catalysts, but also to the development of efficient ...
Mielgo Vicente, María Antonia, Palomo Nicolau, Claudio   +1 more
core   +3 more sources

Cell‐Based Identification of New IDO1 Modulator Chemotypes

Angewandte Chemie, Volume 133, Issue 18, Page 9957-9962, April 26, 2021., 2021
Heme‐competitive indoleamine‐2,3‐dioxygenase (IDO1) small‐molecule modulators are under‐represented as heme displacement is delayed in in vitro assays. This limitation can be overcome by cell‐based screening as employed in this study, which revealed novel chemotypes that potently inhibit IDO1 activity and kynurenine production by competing with heme ...
Elisabeth Hennes, Philipp Lampe, Lara Dötsch, Nora Bruning, Lisa‐Marie Pulvermacher, Sonja Sievers, Slava Ziegler, Herbert Waldmann   +7 more
wiley   +1 more source