Due to the emergence of multidrug-resistant pathogenic microorganisms, the search for novel antimicrobials is urgent. Inspired by marine alkaloids, a series of indolomethyl pyrazino [1,2-]quinazoline-3,6-diones was prepared using a one-pot microwave-assisted multicomponent polycondensation of amino acids. The compounds were evaluated for their antimicrobial activity against a panel of nine bacterial strains and five fungal strains. Compounds 26 and 27 were the most effective against ATCC 29213 reference strain with MIC values of 4 μg mL, and a methicillin-resistant (MRSA) isolate with MIC values of 8 μg mL. It was possible to infer that enantiomer (-)-26 was responsible for the antibacterial activity (MIC 4 μg mL) while (+)-26 had no activity. Furthermore, compound (-)-26 was able to impair biofilm production and no significant cytotoxicity towards differentiated and non-differentiated SH-SY5Y cells was observed. Compounds 26, 28, and 29 showed a weak antifungal activity against clinical isolate with MIC 128 μg mL and presented a synergistic effect with fluconazole.
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http://dx.doi.org/10.1039/d0ra05319h | DOI Listing |
The clinical breakpoint for a drug-pathogen combination reflects the drug susceptibility of the pathogen wild-type population, the location of the infection, the integrity of the host immune response, and the drug-pathogen pharmacokinetic (PK)/pharmacodynamic (PD) relationship. That PK/PD relationship, along with the population variability in drug exposure, is used to determine the probability of target attainment (PTA) of the PK/PD index at a specified minimum inhibitory concentration (MIC) for a selected target value. The PTA is used to identify the pharmacodynamic cutoff value (CO), which is one of the three components used to establish the clinical breakpoint.
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Deraya University, Pharmacognosy, New Minia, New Minia, EGYPT.
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Vietnam National University Hanoi, VNU University of Science, 19 Le Thanh Tong, Hoankiem, VIET NAM.
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