Oxazolidinones as versatile scaffolds in medicinal chemistry

GFS Fernandes, CB Scarim, SH Kim, J Wu… - RSC Medicinal …, 2023 - pubs.rsc.org
Oxazolidinone is a five-member heterocyclic ring with several biological applications in
medicinal chemistry. Among the three possible isomers, 2-oxazolidinone is the most …

Small molecule LpxC inhibitors against gram-negative bacteria: Advances and future perspectives

Z Niu, P Lei, Y Wang, J Wang, J Yang… - European Journal of …, 2023 - Elsevier
Abstract Uridine diphosphate-3-O-(hydroxymyristoyl)-N-acetylglucosamine deacetylase
(LpxC) is a metalloenzyme with zinc ions as cofactors and is a key enzyme in the essential …

Acetylene group, friend or foe in medicinal chemistry

TT Talele - Journal of Medicinal Chemistry, 2020 - ACS Publications
The use of an acetylene (ethynyl) group in medicinal chemistry coincides with the launch of
the Journal of Medicinal Chemistry in 1959. Since then, the acetylene group has been …

Discovery of Novel N-Isoxazolinylphenyltriazinones as Promising Protoporphyrinogen IX Oxidase Inhibitors

DW Wang, RB Zhang, SY Yu, L Liang… - Journal of agricultural …, 2019 - ACS Publications
Protoporphyrinogen oxidase (PPO, EC 1.3. 3.4) is a promising target for herbicide discovery.
Search for new compounds with novel chemotypes is a key objective for agrochemists …

Structure–kinetic relationship studies for the development of long residence time LpxC inhibitors

S Basak, Y Li, S Tao, F Daryaee, J Merino… - Journal of medicinal …, 2022 - ACS Publications
UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC) is a promising
drug target in Gram-negative bacteria. Previously, we described a correlation between the …

Room Temperature Cu-Catalyzed N-Arylation of Oxazolidinones and Amides with (Hetero)Aryl Iodides

S Bhunia, S De, D Ma - Organic Letters, 2022 - ACS Publications
N, N′-Bis (pyridin-2-ylmethyl) oxalamide (BPMO) was found to be an apposite promoter for
the Cu-catalyzed N-arylation of oxazolidinones and primary and secondary amides with …

Rational design, synthesis, molecular modeling, biological activity, and mechanism of action of polypharmacological norfloxacin hydroxamic acid derivatives

AMK El-Sagheir, IA Nekhala… - RSC Medicinal …, 2023 - pubs.rsc.org
Fluoroquinolones are broad-spectrum antibiotics that target gyrase and topoisomerase IV,
involved in DNA compaction and segregation. We synthesized 28 novel norfloxacin …

Discovery of novel inhibitors of LpxC displaying potent in vitro activity against gram-negative bacteria

JP Surivet, P Panchaud, JL Specklin… - Journal of Medicinal …, 2019 - ACS Publications
UDP-3-O-((R)-3-hydroxymyristoyl)-N-glucosamine deacetylase (LpxC) is as an attractive
target for the discovery and development of novel antibacterial drugs to address the critical …

Nitrile Oxide, Alkenes, Dipolar Cycloaddition, Isomerization and Metathesis Involved in the Syntheses of 2-Isoxazolines

S Krompiec, P Lodowski, A Kurpanik-Wójcik, B Gołek… - Molecules, 2023 - mdpi.com
The involvement of 1, 3-dipolar cycloaddition (1, 3-DP), double bond migration, metathesis,
and nitrile oxide (including in situ-generated nitrile oxide) as dipoles, together with the C= C …

Two distinct mechanisms of inhibition of LpxA acyltransferase essential for lipopolysaccharide biosynthesis

W Han, X Ma, CJ Balibar, CM Baxter Rath… - Journal of the …, 2020 - ACS Publications
The lipopolysaccharide biosynthesis pathway is considered an attractive drug target against
the rising threat of multi-drug-resistant Gram-negative bacteria. Here, we report two novel …