Multicomponent reaction toolbox for peptide macrocyclization and stapling
In the past decade, multicomponent reactions have experienced a renaissance as powerful
peptide macrocyclization tools enabling the rapid creation of skeletal complexity and …
peptide macrocyclization tools enabling the rapid creation of skeletal complexity and …
Multicomponent reactions in ligation and bioconjugation chemistry
Conspectus Multicomponent reactions (MCRs) encompass an exciting class of chemical
transformations that have proven success in almost all fields of synthetic organic chemistry …
transformations that have proven success in almost all fields of synthetic organic chemistry …
Peptide bond-forming reaction via amino acid silyl esters: New catalytic reactivity of an aminosilane
W Muramatsu, C Manthena, E Nakashima… - ACS …, 2020 - ACS Publications
The epimerization-free formation of peptide bonds is crucial for the development of peptide
therapeutics and pharmaceuticals. Herein, we report a hydrosilane-mediated approach for …
therapeutics and pharmaceuticals. Herein, we report a hydrosilane-mediated approach for …
Chemical conjugation in drug delivery systems
Cancer is one of the diseases with the highest mortality rate. Treatments to mitigate cancer
are usually so intense and invasive that they weaken the patient to cure as dangerous as the …
are usually so intense and invasive that they weaken the patient to cure as dangerous as the …
The bioorthogonal isonitrile–chlorooxime ligation
RJB Schafer, MR Monaco, M Li, A Tirla… - Journal of the …, 2019 - ACS Publications
Bioorthogonal reactions are valuable tools for the selective labeling and imaging of natural
products and proteins. Here, we present the reaction between isonitriles and chlorooximes …
products and proteins. Here, we present the reaction between isonitriles and chlorooximes …
Exploitation of the Ugi–Joullié reaction in drug discovery and development
S Gazzotti, G Rainoldi, A Silvani - Expert Opinion on Drug …, 2019 - Taylor & Francis
Introduction: Multicomponent reactions are paramount in drug discovery for their ability to
achieve high levels of diversity within the chemical space, generating complex structures …
achieve high levels of diversity within the chemical space, generating complex structures …
Synthesis of Peptide N-Acylpyrroles via Anodically Generated N, O-Acetals
An electrochemical approach to peptide C-terminal N-acylpyrroles is described from readily
accessible C-terminal hydroxyproline-containing peptides, prepared via standard Fmoc …
accessible C-terminal hydroxyproline-containing peptides, prepared via standard Fmoc …
Application of Post-Ugi Transformation Strategies Towards the Synthesis and Functionalization of 2, 5-Diketopiperazines
S Pandey, P Kushwaha - Tetrahedron, 2024 - Elsevier
2, 5-DKP scaffolds are widely used in medicinal chemistry as the basis for many bioactive
compounds. These scaffolds have a wide range of biological properties, offering numerous …
compounds. These scaffolds have a wide range of biological properties, offering numerous …
Efficient one-pot synthesis of enantiomerically pure N-protected-α-substituted piperazines from readily available α-amino acids
M Jida, S Ballet - New Journal of Chemistry, 2018 - pubs.rsc.org
A new pathway towards enantiomerically pure 3-substituted piperazines, bearing a benzyl
protecting group, has been developed in good overall yields (83–92%), starting from …
protecting group, has been developed in good overall yields (83–92%), starting from …
Diversity driven decoration and ligation of fullerene by Ugi and Passerini multicomponent reactions
BB Ravanello, N Seixas… - … A European Journal, 2018 - Wiley Online Library
Aiming at providing an efficient and versatile method for the diversity‐oriented decoration
and ligation of fullerenes, we report the first C60 derivatization strategy based on isocyanide …
and ligation of fullerenes, we report the first C60 derivatization strategy based on isocyanide …