1. New piperazine and morpholine derivatives: Mass spectrometry characterization and evaluation of their antimicrobial activity.
- Author
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Acquavia MA, Bonomo MG, Bianco G, Salzano G, Gaeta C, Iannece P, Di Capua A, Giuzio F, and Saturnino C
- Subjects
- Gram-Positive Bacteria drug effects, Structure-Activity Relationship, Piperazine pharmacology, Piperazine chemistry, Morpholines pharmacology, Morpholines chemistry, Anti-Bacterial Agents pharmacology, Anti-Bacterial Agents chemistry, Anti-Bacterial Agents analysis, Anti-Bacterial Agents chemical synthesis, Microbial Sensitivity Tests methods, Piperazines pharmacology, Piperazines chemistry, Gram-Negative Bacteria drug effects, Mass Spectrometry methods
- Abstract
Recently, pharmaceutical research has been focused on the design of new antibacterial drugs with higher selectivity towards several strains. Major issues concern the possibility to obtain compounds with fewer side effects, at the same time effectively overcoming the problem of antimicrobial resistance. Several solutions include the synthesis of new pharmacophores starting from piperazine or morpholine core units. Mass spectrometry-based techniques offer important support for the structural characterization of newly synthesized compounds to design safer and more effective drugs for various medical conditions. Here, two new piperazine derivatives and four new morpholine derivatives were synthesized and structurally characterized through a combined approach of Fourier transform-ion cyclotron resonance (FT-ICR) and Linear Trap Quadrupole (LTQ) mass spectrometry. The support of both high-resolution and low-resolution mass spectrometric data namely accurate mass measurements, isotopic distribution and MS
n spectra, was crucial to confirm the success of the synthesis. These compounds were further evaluated for inhibitory activity against a total of twenty-nine Gram-positive and Gram-negative bacteria to determine the action spectrum and the antimicrobial effectiveness. Results demonstrated compounds' antimicrobial activity against many tested bacterial species, providing an inhibitory effect linked to different chemical structure and suggesting that the new-synthesized derivatives could be considered as promising antimicrobial agents., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier B.V. All rights reserved.)- Published
- 2024
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