An update on the nitrogen heterocycle compositions and properties of US FDA-approved pharmaceuticals (2013–2023)

CM Marshall, JG Federice, CN Bell… - Journal of Medicinal …, 2024 - ACS Publications
This Perspective is a continuation of our analysis of US FDA-approved small-molecule drugs
(1938–2012) containing nitrogen heterocycles. In this study we report drug structure and …

Deuterium in drug discovery: progress, opportunities and challenges

RMC Di Martino, BD Maxwell, T Pirali - Nature Reviews Drug Discovery, 2023 - nature.com
Substitution of a hydrogen atom with its heavy isotope deuterium entails the addition of one
neutron to a molecule. Despite being a subtle change, this structural modification, known as …

Recent developments for the deuterium and tritium labeling of organic molecules

S Kopf, F Bourriquen, W Li, H Neumann… - Chemical …, 2022 - ACS Publications
Organic compounds labeled with hydrogen isotopes play a crucial role in numerous areas,
from materials science to medicinal chemistry. Indeed, while the replacement of hydrogen by …

US FDA approved drugs from 2015–June 2020: a perspective

P Bhutani, G Joshi, N Raja, N Bachhav… - Journal of Medicinal …, 2021 - ACS Publications
In the present work, we report compilation and analysis of 245 drugs, including small and
macromolecules approved by the US FDA from 2015 until June 2020. Nearly 29% of the …

C–H deuteration of organic compounds and potential drug candidates

G Prakash, N Paul, GA Oliver, DB Werz… - Chemical Society …, 2022 - pubs.rsc.org
C–H deuteration has been intricately developed to satisfy the urgent need for site-selectively
deuterated organic frameworks. Deuteration has been primarily used to study kinetic isotope …

Borrowing hydrogen for organic synthesis

BG Reed-Berendt, DE Latham, MB Dambatta… - ACS Central …, 2021 - ACS Publications
Borrowing hydrogen is a process that is used to diversify the synthetic utility of commodity
alcohols. A catalyst first oxidizes an alcohol by removing hydrogen to form a reactive …

Facile and general electrochemical deuteration of unactivated alkyl halides

P Li, C Guo, S Wang, D Ma, T Feng, Y Wang… - Nature …, 2022 - nature.com
Herein, a facile and general electroreductive deuteration of unactivated alkyl halides (X= Cl,
Br, I) or pseudo-halides (X= OMs) using D2O as the economical deuterium source was …

Organo‐Mediator Enabled Electrochemical Deuteration of Styrenes

K Yang, T Feng, Y Qiu - Angewandte Chemie International …, 2023 - Wiley Online Library
Despite widespread use of the deuterium isotope effect, selective deuterium labeling of
chemical molecules remains a major challenge. Herein, a facile and general …

Radical deuteration

N Li, Y Li, X Wu, C Zhu, J Xie - Chemical Society Reviews, 2022 - pubs.rsc.org
Deuterated chemicals are becoming irreplaceable in pharmaceutical engineering, material
science and synthetic chemistry. Many excellent reviews have discussed acid/base …

An orally available Mpro inhibitor is effective against wild-type SARS-CoV-2 and variants including Omicron

BX Quan, H Shuai, AJ Xia, Y Hou, R Zeng, XL Liu… - Nature …, 2022 - nature.com
Emerging SARS-CoV-2 variants continue to cause waves of new infections globally.
Developing effective antivirals against SARS-CoV-2 and its variants is an urgent task. The …