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Frontispiece: Protein‐Templated Hit Identification through an Ugi Four‐Component Reaction
Author(s) -
Mancini Federica,
Unver M. Yagiz,
Elgaher Walid A. M.,
Jumde Varsha R.,
Alhayek Alaa,
Lukat Peer,
Herrmann Jennifer,
Witte Martin D.,
Köck Matthias,
Blankenfeldt Wulf,
Müller Rolf,
Hirsch Anna K. H.
Publication year - 2020
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.202086462
Subject(s) - ugi reaction , component (thermodynamics) , chemistry , combinatorial chemistry , in situ , stereochemistry , isocyanide , organic chemistry , physics , thermodynamics
The Ugi four‐component reaction (Ugi‐4CR) was employed as a new reaction in kinetic target‐guided synthesis (KTGS). Applying the reaction on the bacterial β sliding clamp (DnaN) (middle) resulted in marked acceleration of product assembly from a library of eight building blocks representing four chemical classes. UPLC‐HRMS analysis of the in situ Ugi‐4CR in the presence of the strong inhibitor griselimycin (left) or using endothiapepsin (right) as an unrelated protein revealed no product formation, demonstrating the specificity of the DnaN‐templated reaction. For more details see the Full paper by A. K. H. Hirsch et al. on page 14585 ff.