Autor(es):
Ferraz, Ricardo ; Silva, Dário ; Dias, Ana Rita ; Dias, Vitorino ; Santos, Miguel M. ; Pinheiro, Luís ; Prudêncio, Cristina ; Noronha, João Paulo ; Petrovski, Željko ; Branco, Luís C.
Data: 2020
Identificador Persistente: http://hdl.handle.net/10400.22/16261
Origem: Repositório Científico do Instituto Politécnico do Porto
Projeto/bolsa:
info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB/50006/2020/PT;
Assunto(s): Active pharmaceutical; Sensitive bacteria; penicillin G; Amoxicillin hydrolysate derivatives
Descrição
The preparation and characterization of ionic liquids and organic salts (OSILs) that contain anionic penicillin G [secoPen] and amoxicillin [seco-Amx] hydrolysate derivatives and their in vitro antibacterial activity against sensitive and resistant Escherichiacoli and Staphylococcusaureus strains is reported. Eleven hydrolyzed β-lactam-OSILs were obtained after precipitation in moderate-to-high yields via the neutralization of the basic ammonia buffer of antibiotics with different cation hydroxide salts. The obtained minimum inhibitory concentration (MIC) data of the prepared compounds showed a relative decrease of the inhibitory concentrations (RDIC) in the order of 100 in the case of [C2OHMIM][seco-Pen] against sensitive S. aureus ATCC25923 and, most strikingly, higher than 1000 with [C16Pyr][seco-Amx] against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300. These outstanding in vitro results showcase that a straightforward transformation of standard antibiotics into hydrolyzed organic salts can dramatically change the pharmaceutical activity of a drug, including giving rise to potent formulations of antibiotics against deadly bacteria strains.
