Synthesis and Antibacterial Activity of Ionic Liquids and Organic Salts Based on Penicillin G and Amoxicillin hydrolysate Derivatives against Resistant Bacteria

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 and strains is reported. Eleven hydrolyzed β-lactam...

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Bibliographic Details
Published in:	Pharmaceutics 2020-03, Vol.12 (3), p.221
Main Authors:	Ferraz, Ricardo, Silva, Dário, Dias, Ana Rita, Dias, Vitorino, Santos, Miguel M, Pinheiro, Luís, Prudêncio, Cristina, Noronha, João Paulo, Petrovski, Željko, Branco, Luís C
Format:	Article
Language:	eng
Subjects:	active pharmaceutical ingredients-ionic liquids and organic salts (api-osils) penicillin g and amoxicillin hydrolysate derivatives resistant bacteria sensitive bacteria
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Summary:	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 and 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 [C OHMIM][seco-Pen] against sensitive ATCC25923 and, most strikingly, higher than 1000 with [C Pyr][seco-Amx] against methicillin-resistant (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.
ISSN:	1999-4923 1999-4923