Document Report Card
Basic Information
ID: ALA4138160
Journal: Eur J Med Chem
Title: Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
Authors: Hagras M, Hegazy YA, Elkabbany AH, Mohammad H, Ghiaty A, Abdelghany TM, Seleem MN, Mayhoub AS.
Abstract: A new series of oxadiazolylbiphenylthiazoles was prepared with the objective of improving the limited solubility of first-generation derivatives while maintaining antibacterial activity against drug-resistant Staphylococcus aureus. Studying the structure-activity relationship at the cationic part provided the piperazine-1-carboximidamide derivative 27 with a MIC (MRSA) value of 1.1 μg/mL, bactericidal mode of action, and a 50-fold improvement in aqueous solubility. Additionally, 27 exhibited a wider safety margin against mammalian cells, and most importantly, a significant improvement in oral bioavailability.
CiteXplore: 29126738