Chan, Kin-Fai published the artcileEfficient Synthesis of Amine-Linked 2,4,6-Trisubstituted Pyrimidines as a New Class of Bacterial FtsZ Inhibitors, Quality Control of 87179-40-6, the publication is ACS Omega (2017), 2(10), 7281-7292, database is CAplus and MEDLINE.
We have recently identified a new class of FtsZ-interacting compounds that possess a 2,4,6-trisubstituted pyrimidine-quinuclidine scaffold with moderate antibacterial activity. Employing this scaffold as a mol. template, a compound library of amine-linked 2,4,6-trisubstituted pyrimidines with ninety-nine candidates was successfully established by employing an efficient convergent synthesis designed to explore its structure activity relationship. The results of min. inhibitory concentration (MIC) assay against S. aureus strains and cytotoxicity assay against mouse L929 cell line identified those compounds with potent anti-staphylococcal properties (MIC ranges from 3 to 8 μg/mL) and some extent of cytotoxicity against normal cell (IC50 ranges from 6 to 27 μM). Importantly, three compounds also exhibited potent antibacterial activities against nine clin. isolated MRSA strains. One of the compounds, I, exhibited low spontaneous frequency of resistance, low toxicity against G. mellonella larvae as well as the ability to rescue G. mellonella larvae (20% survival rate at dosage of 100 mg/Kg) infected with LD of MRSA ATCC 43300 strain. Biol. characterization of compound I by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purified S. aureus FtsZ protein verified that it interacted with the FtsZ protein. Such property of FtsZ inhibitor was further confirmed by observations of iconic filamentous cell phenotype and mislocalization of the Z-ring formation of B. subtilis. Taken together, these 2,4,6-trisubstituted pyrimidine derivatives represent a novel scaffold of S. aureus FtsZ inhibitors.
ACS Omega published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Quality Control of 87179-40-6.
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