Synthesis, lipophilicity and antimicrobial activity evaluation of some new thiazolyl-oxadiazolines.

Autor: Stoica CI; Therapeutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania., IonuȚ I; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania., Pîrnău A; Molecular and Biomolecular Physics Department, National Institute for Research and Development of Isotopic and Molecular Technologies, Cluj-Napoca, Romania., Pop C; Food Science and Technology Department, University of Agricultural Sciences and Veterinary Medicine, Cluj-Napoca, Romania., Rotar A; Food Science and Technology Department, University of Agricultural Sciences and Veterinary Medicine, Cluj-Napoca, Romania., Vlase L; Pharmaceutical Technology and Biopharmaceutics Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania., Oniga S; Therapeutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania., Oniga O; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.
Jazyk: angličtina
Zdroj: Clujul medical (1957) [Clujul Med] 2015; Vol. 88 (4), pp. 521-9. Date of Electronic Publication: 2015 Nov 15.
DOI: 10.15386/cjmed-473
Abstrakt: Background and Aims: Synthesis of new potential antimicrobial agents and evaluation of their lipophilicity.
Methods: Ten new thiazolyl-oxadiazoline derivatives were synthesized and their structures were validated by 1H-NMR and mass spectrometry. The lipophilicity of the compounds was evaluated using the principal component analysis (PCA) method. The necessary data for applying this method were obtained by reverse-phase thin-layer chromatography (RP-TLC). The antimicrobial activities were tested in vitro against four bacterial strains and one fungal strain.
Results: The lipophilicity varied with the structure but could not be correlated with the antimicrobial activity, since this was modest.
Conclusions: We have synthesized ten new heterocyclic compounds. After their physical and chemical characterization, we determined their lipophilicity and screened their antimicrobial activity.
Databáze: MEDLINE
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