4.6 Article

Bioactivity of Isostructural Hydrogen Bonding Frameworks Built from Pipemidic Acid Metal Complexes

Journal

MOLECULES
Volume 25, Issue 10, Pages -

Publisher

MDPI
DOI: 10.3390/molecules25102374

Keywords

mechanochemistry; bioactivity; pipemidic acid; antibiotics

Funding

  1. Fundacao para a Ciencia e a Tecnologia (FCT, Portugal) [UIDB/00100/2020, UIDP/00100/2020, PTDC/QUI-OUT/30988/2017, 57/2016, CEECIND/02001/2017]
  2. FEDER, Portugal2020
  3. FEDER, Lisboa2020 [LISBOA-01-0145-FEDER-030988]
  4. Fundação para a Ciência e a Tecnologia [PTDC/QUI-OUT/30988/2017] Funding Source: FCT

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We report herein three novel complexes whose design was based on the approach that consists of combining commercially available antibiotics with metals to attain different physicochemical properties and promote antimicrobial activity. Thus, new isostructural three-dimensional (3D) hydrogen bonding frameworks of pipemidic acid with manganese (II), zinc (II) and calcium (II) have been synthesised by mechanochemistry and are stable under shelf conditions. Notably, the antimicrobial activity of the compounds is maintained or even increased; in particular, the activity of the complexes is augmented against Escherichia coli, a representative of Gram-negative bacteria that have emerged as a major concern in drug resistance. Moreover, the synthesised compounds display similar general toxicity (Artemia salina model) levels to the original antibiotic, pipemidic acid. The increased antibacterial activity of the synthesised compounds, together with their appropriate toxicity levels, are promising outcomes.

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