English
norskBlar i forfatter "Engqvist, Magnus"
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Amphipathic Barbiturates as Mimics of Antimicrobial Peptides and the Marine Natural Products Eusynstyelamides with Activity against Multi-resistant Clinical Isolates
(Journal article; Tidsskriftartikkel; Peer reviewed, 2021-07-27)We report a series of synthetic cationic amphipathic barbiturates inspired by the pharmacophore model of small antimicrobial peptides (AMPs) and the marine antimicrobials eusynstyelamides. These N,N′-dialkylated-5,5-disubstituted barbiturates consist of an achiral barbiturate scaffold with two cationic groups and two lipophilic side chains. Minimum inhibitory concentrations of 2–8 μg/mL were achieved ... -
Antimicrobial activity of amphipathic α,α-disubstituted β-amino amide derivatives against ESBL–CARBA producing multi-resistant bacteria; effect of halogenation, lipophilicity and cationic character
(Journal article; Tidsskriftartikkel; Peer reviewed, 2019-09-06)The rapid emergence and spread of multi-resistant bacteria have created an urgent need for new antimicrobial agents. We report here a series of amphipathic α,α-disubstituted β-amino amide derivatives with activity against 30 multi-resistant clinical isolates of Gram-positive and Gram-negative bacteria, including isolates with extended spectrum β-lactamase – carbapenemase (ESBL-CARBA) production. A ... -
Efficient and scalable synthesis of α,α-disubstituted β-amino amides
(Journal article; Tidsskriftartikkel; Peer reviewed, 2016-07-12)A practical and efficient methodology for the preparation of 2-aminoethyl α,α-disubstituted β-amino amides in three steps from methyl cyanoacetate has been developed. The key step in the synthesis was the chemoselective reduction of the nitrile group in presence of an amide and aryl halide functionalities. Reduction with RANEY® Nickel catalyst, either with molecular hydrogen (8–10 bar) or under ... -
Palladium(0)-Catalyzed Cross-Couplings of 2-Bromophosphinine
(Journal article; Tidsskriftartikkel; Peer reviewed, 2013-05-21)A new Negishi-type cross-coupling of 2-bromophosphinine has been developed. The new method expands the scope of palladium-catalyzed couplings to monobromophosphinines, which have been considered as poor substrates so far. Moreover, aryl-, alkenyl-, and alkynylzinc bromides were found to be effective coupling partners.
