Results 21 to 30 of about 2,043,921 (203)

Protein-Templated Hit Identification via an Ugi Four-Component Reaction [PDF]

, 2020
Kinetic target-guided synthesis represents an efficient hit-identification strategy, in which the protein assembles its own inhibitors from a pool of building blocks via an irreversible reaction.
jennifer, herrmann, Martin D., Witte, Matthias, Köck, M. Yagiz, Unver, Varsha R., Jumde, Peer, Lukat, rolf, müller, Wulf, Blankenfeldt, Federica, Mancini, Anna K.H., Hirsch, Walid, Elgaher, Alaa, Alhayek   +11 more
core   +3 more sources

Propargyl Amines: Versatile Building Blocks in Post‐Ugi Transformations

ChemistryOpen, 2023
The Ugi reaction, a multicomponent reaction, allows diversity‐oriented synthesis Its importance is recognized by an exponential increase in the publications utilizing the post‐Ugi transformations as a strategy to build complex molecules via simple and ...
Rinkal B. Bhoraniya, Dr. Sachin G. Modha
doaj   +1 more source

Ugi Four-Component Reactions Using Alternative Reactants

Molecules, 2023
The Ugi four-component reaction (Ugi-4CR) undoubtedly is the most prominent multicomponent reaction (MCRs) that has sparked organic chemists’ interest in the field.
Seyyed Emad Hooshmand, Wei Zhang
doaj   +1 more source

Engineered Transformer Base Editor with Enhanced Editing Efficiency. [PDF]

Adv Sci (Weinh)
A highly efficient transformer base editor system achieves robust genomic editing in a humanized mouse model. This work establishes a versatile and translatable platform, opening new avenues for precision gene therapy. ABSTRACT Canonical cytosine base editors (CBEs) achieve precise C‐to‐T conversions without inducing DNA double‐strand breaks (DSBs ...
Chen B, Liang L, Xu R, Wang T, Chen H, Lu D.   +5 more
europepmc   +2 more sources

The Ugi-Smiles Reaction on Steroids: Discovery of Bioactive N,N-Disubstituted 3- Aminoestrones [PDF]

, 2020
The Ugi-Smiles multicomponent reaction is a powerful tool for obtaining N-arylamines from acidic phenols and has been widely used for gaining access to structurally diverse scaffolds. In this work we demonstrate that this isocyanide-based coupling can be
Evelyn, Bonifazi, Javier Alberto, Ramirez, Cecilia, Attorresi, Bruno, Falcone, Gabriel, Gola, Andrea, Barquero   +5 more
core   +1 more source

Strain and Complexity, Passerini and Ugi Reactions of Four‐Membered Heterocycles and Further Elaboration of TOSMIC Product

ChemistryOpen, 2023
Straightforward and general Passerini and Ugi procedures have been developed to incorporate four‐membered heterocycles into highly functionalized scaffolds.
Gábor Sztanó, Dr. Zoltán Dobi, Dr. Tibor Soós   +2 more
doaj   +1 more source

Controlling the stereochemistry in 2-oxo-aldehyde-derived Ugi adducts through the cinchona alkaloid-promoted electrophilic fluorination

Beilstein Journal of Organic Chemistry, 2020
In this report, we introduce a new strategy for controlling the stereochemistry in Ugi adducts. Instead of controlling stereochemistry directly during the Ugi reaction we have attempted to stereodefine the chiral center at the peptidyl position through ...
Yuqing Wang, Gaigai Wang, Anatoly A. Peshkov, Ruwei Yao, Muhammad Hasan, Manzoor Zaman, Chao Liu, Stepan Kashtanov, Olga P. Pereshivko, Vsevolod A. Peshkov   +9 more
doaj   +1 more source

Regioselective Cyclic Iminium Formation of Ugi Advanced Intermediates: Rapid Access to 3,4-Dihydropyrazin-2(1H)-ones and Other Diverse Nitrogen-Containing Heterocycles

Molecules, 2023
Herein, advanced intermediates were synthesized through Ugi four-component reactions of isocyanides, aldehydes, masked amino aldehyde, and carboxylic acids, including N-protected amino acids.
Naděžda Cankařová, Viktor Krchňák
doaj   +1 more source

Temperature-Controlled Diastereoselective Doebner/Ugi Tandem Reaction

SynOpen, 2023
Novel peptidomimetics containing a pyrrolone fragment were synthesized by a tandem combination of Doebner and Ugi type multicomponent reactions with controlled diastereoselectivity. This approach represents a convenient synthesis in the temperature range
Yana Sakhno, Oleksandr Radchenko, Vyacheslav Saraev, Yuliia Shliapkina, Mariia Kaidash, Mariia Shyshkina, Svitlana Shishkina, Vladimir Musatov, Sergey Desenko, Valentyn Chebanov   +9 more
doaj   +1 more source

Synthesis and Evaluation of Peptoid-Based Compound Libraries as Inhibitors of Parasite Metallo-Aminopeptidases. [PDF]

ChemMedChem
Evaluation of two libraries of peptoid‐based compounds for inhibitory activity against PfA‐M1 from Plasmodium falciparum, TcLAP from Trypanosoma cruzi, and LmLAP from Leishmania major reveals the crucial role of hydrophobic interactions in the inhibition process of these parasite metallo‐aminopeptidases.
Aguado ME, Ojeda-Carralero GM, Rodríguez MA, Rúa I, Guerra H, Hernández EB, Coppola G, Alberti S, Rodríguez A, Izquierdo M, Betzel C, Pettazzi F, Coro-Bermello J, Eycken EVV, Westermann B, González-Bacerio J, Rivera DG.   +16 more
europepmc   +2 more sources