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ABSTRACT:
SUBMITTER: Hagras M
PROVIDER: S-EPMC5736435 | biostudies-literature | 2018 Jan
REPOSITORIES: biostudies-literature
Hagras Mohamed M Hegazy Youssef A YA Elkabbany Amr H AH Mohammad Haroon H Ghiaty Adel A Abdelghany Tamer M TM Seleem Mohamed N MN Mayhoub Abdelrahman S AS
European journal of medicinal chemistry 20171019
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 w ...[more]