scholarly journals Improved Diazo-Transfer Reaction for DNA-Encoded Chemistry and Its Potential Application for Macrocyclic DEL-Libraries

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1790
Author(s):  
Selahattin Ede ◽  
Mandy Schenk ◽  
Donald Bierer ◽  
Hilmar Weinmann ◽  
Keith Graham
Keyword(s):  
Drug Discovery ◽  
Potential Application ◽  
Medicinal Chemistry ◽  
Transfer Reaction ◽  
Transfer Reactions ◽  
Primary Amines ◽  
Proof Of Concept ◽  
Diazo Transfer Reaction

DNA-encoded libraries (DEL) are increasingly being used to identify new starting points for medicinal chemistry in drug discovery. Herein, we discuss the development of methods that allow the conversion of both primary amines and anilines, attached to DNA, to their corresponding azides in excellent yields. The scope of these diazo-transfer reactions was investigated, and a proof-of-concept has been devised to allow for the synthesis of macrocycles on DNA.

A ‘sulfonyl-azide-free’ (SAFE) aqueous-phase diazo transfer reaction for parallel and diversity-oriented synthesis

2019 ◽  
Vol 55 (36) ◽  
pp. 5239-5242 ◽  
Author(s):  
Dmitry Dar’in ◽  
Grigory Kantin ◽  
Mikhail Krasavin
Keyword(s):  
Aqueous Phase ◽  
Transfer Reaction ◽  
Transfer Reactions ◽  
Diversity Oriented Synthesis ◽  
Sulfonyl Azides ◽  
Sulfonyl Azide ◽  
Diazo Transfer Reaction

Diazo transfer reactions are notoriously associated with the use of potentially explosive sulfonyl azides. Handling of the latter can be avoided with the use of this new protocol.

Trifluoromethyl Ethers and –Thioethers as Tools for Medicinal Chemistry and Drug Discovery

2014 ◽  
Vol 14 (7) ◽  
pp. 941-951 ◽  
Author(s):  
Gregory Landelle ◽  
Armen Panossian ◽  
Frederic Leroux
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry

scholarly journals John Macor is Awarded the 2020 IUPAC-Richter Prize

2020 ◽  
Vol 42 (2) ◽  
pp. 25-25
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry

Abstract The 2020 IUPAC-Richter Prize in Medicinal Chemistry has been awarded to John Macor, PhD, Global Head Integrated Drug Discovery, Sanofi.

Nonclassical oxygen atom transfer reactions of an eight-coordinate dioxomolybdenum(vi) complex

2021 ◽  
Author(s):  
Leila G. Ranis ◽  
Jacqueline Gianino ◽  
Justin M. Hoffman ◽  
Seth N. Brown
Keyword(s):  
Oxygen Atom ◽  
Transfer Reaction ◽  
Transfer Reactions ◽  
Atom Transfer ◽  
Oxygen Atom Transfer ◽  
Oxygen Atom Transfer Reactions ◽  
Atom Transfer Reactions ◽  
Oxygen Atoms

Eight-coordinate MoO2(DOPOQ)2 can donate two oxygen atoms to substrates such as phosphines in a four-electron nonclassical oxygen atom transfer reaction.

scholarly journals Electron transfer studies of a conventional redox probe in human sweat and saliva bio-mimicking conditions

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
P. Krishnaveni ◽  
V. Ganesh
Keyword(s):  
Electron Transfer ◽  
Crystalline Phase ◽  
Liquid Crystalline ◽  
Transfer Reaction ◽  
Electron Transfer Reaction ◽  
Redox Couple ◽  
Liquid Crystalline Phase ◽  
Transfer Reactions ◽  
Redox Probe ◽  
Human Sweat

AbstractModern day hospital treatments aim at developing electrochemical biosensors for early diagnosis of diseases using unconventional human bio-fluids like sweat and saliva by monitoring the electron transfer reactions of target analytes. Such kinds of health care diagnostics primarily avoid the usage of human blood and urine samples. In this context, here we have investigated the electron transfer reaction of a well-known and commonly used redox probe namely, potassium ferro/ferri cyanide by employing artificially simulated bio-mimics of human sweat and saliva as unconventional electrolytes. Typically, electron transfer characteristics of the redox couple, [Fe(CN)6]3−/4− are investigated using electrochemical techniques like cyclic voltammetry and electrochemical impedance spectroscopy. Many different kinetic parameters are determined and compared with the conventional system. In addition, such electron transfer reactions have also been studied using a lyotropic liquid crystalline phase comprising of Triton X-100 and water in which the aqueous phase is replaced with either human sweat or saliva bio-mimics. From these studies, we find out the electron transfer reaction of [Fe(CN)6]3−/4− redox couple is completely diffusion controlled on both Au and Pt disc shaped electrodes in presence of sweat and saliva bio-mimic solutions. Moreover, the reaction is partially blocked by the presence of lyotropic liquid crystalline phase consisting of sweat and saliva bio-mimics indicating the predominant charge transfer controlled process for the redox probe. However, the rate constant values associated with the electron transfer reaction are drastically reduced in presence of liquid crystalline phase. These studies are essentially carried out to assess the effect of sweat and saliva on the electrochemistry of Fe2+/3+ redox couple.

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