scholarly journals On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors

2020 ◽  
Vol 11 (11) ◽  
pp. 1275-1284
Author(s):  
Vinicius Bonatto ◽  
Pedro Henrique Jatai Batista ◽  
Lorenzo Cianni ◽  
Daniela De Vita ◽  
Daniel G. Silva ◽  
...  
Keyword(s):  
Intrinsic Reactivity ◽  
Cruzain Inhibitors

Aldehyde peptide like compounds display a bivalent reactive profile and improved antichagasic potency.

scholarly journals Titelbild: Catalyst-Enabled Site-Divergent Stereoselective Michael Reactions: Overriding Intrinsic Reactivity of Enynyl Carbonyl Acceptors (Angew. Chem. 17/2018)

2018 ◽  
Vol 130 (17) ◽  
pp. 4519-4519
Author(s):  
Daisuke Uraguchi ◽  
Ryo Shibazaki ◽  
Naoya Tanaka ◽  
Kohei Yamada ◽  
Ken Yoshioka ◽  
...  
Keyword(s):  
Michael Reactions ◽  
Intrinsic Reactivity

scholarly journals Synergistic Experimental and Computational Investigation of the Bioorthogonal Reactivity of Substituted Aryltetrazines

2021 ◽  
Author(s):  
Umberto Battisti ◽  
Rocío García-Vázquez ◽  
Dennis Svatunek ◽  
Barbara Herrmann ◽  
Andreas Löffler ◽  
...  
Keyword(s):  
Kinetic Study ◽  
Solvent Effects ◽  
Rate Constants ◽  
Biomedical Applications ◽  
Aqueous Systems ◽  
Phenyl Substituent ◽  
Computational Investigation ◽  
Radiation Burden ◽  
Intrinsic Reactivity

Tetrazines (Tz) have been applied as bioorthogonal agents for various biomedical applications including pretargeted imaging approaches. In radioimmunoimaging, pretargeting increases the target-to-background ratio while simultaneously reducing the radiation burden. We have recently reported a strategy to directly 18F-label highly reactive tetrazines based on a 3-(3-fluorophenyl)-Tz core structure. Herein, we report a kinetic study on this versatile scaffold. A library of 40 different tetrazines was prepared, fully characterized, and investigated with emphasis on second order rate constants for the reaction with trans-cyclooctene (TCO). Our results reveal the effects of various substitution patterns and moreover demonstrate the importance of measuring reactivities in the solvent of interest, as click rates in different solvents do not necessarily correlate well. In particular, we report that tetrazines modified in 2-position of the phenyl substituent show high intrinsic reactivity towards TCO, which is diminished in aqueous systems by unfavorable solvent effects. The obtained results enable the prediction of the bioorthogonal reactivity and thereby facilitate the development of the next-generation of substituted aryltetrazines for in vivo application.

scholarly journals How Prebiotic Chemistry and Early Life Chose Phosphate

Life ◽  
2019 ◽  
Vol 9 (1) ◽  
pp. 26 ◽  
Author(s):  
Ziwei Liu ◽  
Jean-Christophe Rossi ◽  
Robert Pascal
Keyword(s):  
Chemical Evolution ◽  
Early Life ◽  
Prebiotic Chemistry ◽  
Protein Biosynthesis ◽  
Phosphate Esters ◽  
Early Stages ◽  
Mixed Anhydrides ◽  
Living Organisms ◽  
Intrinsic Reactivity ◽  
Thermodynamic Instability

The very specific thermodynamic instability and kinetic stability of phosphate esters and anhydrides impart them invaluable properties in living organisms in which highly efficient enzyme catalysts compensate for their low intrinsic reactivity. Considering their role in protein biosynthesis, these properties raise a paradox about early stages: How could these species be selected in the absence of enzymes? This review is aimed at demonstrating that considering mixed anhydrides or other species more reactive than esters and anhydrides can help in solving the paradox. The consequences of this approach for chemical evolution and early stages of life are analysed.

scholarly journals Intrinsic reactivity of a uranium metallacyclopropene toward unsaturated organic molecules

2016 ◽  
Vol 45 (41) ◽  
pp. 16441-16452 ◽  
Author(s):  
Lei Zhang ◽  
Bo Fang ◽  
Guohua Hou ◽  
Lin Ai ◽  
Wanjian Ding ◽  
...  
Keyword(s):  
Electron Transfer ◽  
Small Molecules ◽  
Organic Molecules ◽  
Transfer Processes ◽  
Electron Transfer Processes ◽  
Intrinsic Reactivity

A uranium metallacyclopropene shows a rich chemistry in the activation of small molecules by two electron transfer processes.

scholarly journals Molecular Design, Synthesis and Trypanocidal Activity of Dipeptidyl Nitriles as Cruzain Inhibitors

2015 ◽  
Vol 9 (7) ◽  
pp. e0003916 ◽  
Author(s):  
Leandro A. A. Avelar ◽  
Cristian D. Camilo ◽  
Sérgio de Albuquerque ◽  
William B. Fernandes ◽  
Cristiana Gonçalez ◽  
...  
Keyword(s):  
Molecular Design ◽  
Design Synthesis ◽  
Trypanocidal Activity ◽  
Cruzain Inhibitors

scholarly journals Cover Picture: Catalyst-Enabled Site-Divergent Stereoselective Michael Reactions: Overriding Intrinsic Reactivity of Enynyl Carbonyl Acceptors (Angew. Chem. Int. Ed. 17/2018)

2018 ◽  
Vol 57 (17) ◽  
pp. 4431-4431
Author(s):  
Daisuke Uraguchi ◽  
Ryo Shibazaki ◽  
Naoya Tanaka ◽  
Kohei Yamada ◽  
Ken Yoshioka ◽  
...  
Keyword(s):  
Michael Reactions ◽  
Intrinsic Reactivity

Intrinsic reactivity of biomass-derived char under steam gasification conditions-potential of wood ash as catalyst

2013 ◽  
Vol 217 ◽  
pp. 289-299 ◽  
Author(s):  
Pavlina Nanou ◽  
Héctor E. Gutiérrez Murillo ◽  
Wim P.M. van Swaaij ◽  
Guus van Rossum ◽  
Sascha R.A. Kersten
Keyword(s):  
Wood Ash ◽  
Steam Gasification ◽  
Intrinsic Reactivity
Sign in / Sign up

Export Citation Format

Share Document