Inhibition of the Antibiotic Activity of Cephalosporines by Co-Crystallization with Thymol
2022
academicJournal
Zugriff:
Three structurally similar antibiotics of the cephalosporin (CEPH) class, namely, cephalexin (CPX), cephradine (CFD), and cefaclor (CFC), have been co-crystallized with thymol (THY) via different preparation techniques, yielding the hydrated co-crystals CPX·THY·2.5H 2 O form I and form II, CFD·THY·2.5H 2 O, and CFC·THY·4H 2 O. All co-crystals were structurally characterized by single crystal and/or powder X-ray diffraction. In all co-crystals, except in the case of the elusive metastable form I of CPX·THY·2.5H 2 O, the CEPH molecules interact with thymol only via water bridges; i.e., there is no direct hydrogen bonding between CEPH molecules and THY. Preliminary antimicrobial experiments via measurements of minimal inhibitory concentration (MIC) provide clear-cut evidence that the association with thymol increases the resistance of both Gram-negative and Gram-positive bacteria to the antibiotic with respect to pure CEPH as well as to physical mixtures of CEPH with thymol.
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Inhibition of the Antibiotic Activity of Cephalosporines by Co-Crystallization with Thymol
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Autor/in / Beteiligte Person: | Cecilia Fiore (9336724) ; Alessandra Baraghini (11986586) ; Oleksii Shemchuk (3355310) ; Vittorio Sambri (92790) ; Manuela Morotti (11986589) ; Fabrizia Grepioni (1492783) ; Dario Braga (1492780) |
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Veröffentlichung: | 2022 |
Medientyp: | academicJournal |
DOI: | 10.1021/acs.cgd.1c01435.s001 |
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