Rh -Catalyzed De-symmetrization of Ethane-1,2-dithiol and Propane-1,3-dithiol Yields Metallo-β-lactamase Inhibitors

Overview

Journal ChemMedChem

Specialties Chemistry
Pharmacology

Date 2021 Jun 29

PMID 34184833

Citations 6

Authors

Mikhail Krasavin

Daniil Zhukovsky

Igor Solovyev

Darina Barkhatova

Dmitry Darin

Denia Frank

Giada Martinelli

Lilia Weizel

Anna Proschak

Marco Rotter

Jan S Kramer

Steffen Brunst

Thomas A Wichelhaus

Ewgenij Proschak

Affiliations

Soon will be listed here.

Abstract

Diversity-oriented synthesis (DOS) is a rich source for novel lead structures in Medicinal Chemistry. In this study, we present a DOS-compatible method for synthesis of compounds bearing a free thiol moiety. The procedure relies on Rh(II)-catalyzed coupling of dithiols to diazo building blocks. The synthetized library was probed against metallo-β-lactamases (MBLs) NDM-1 and VIM-1. Biochemical and biological evaluation led to identification of novel potent MBL inhibitors with antibiotic adjuvant activity.

Citing Articles

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