The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Apr. 24, 2018
Filed:
Sep. 29, 2016
The Hong Kong Polytechnic University, Hong Kong, CN;
The Royal Institution for the Advancement of Learning / Mcgill University, Montreal, CA;
Abstract
Filamenting temperature-sensitive mutant Z (FtsZ) protein plays a crucial role in the bacterial cell division machinery and is a validated drug target for antibacterial agents. The present invention relates to FtsZ-interacting compounds that possess a 2,4,6-trisubstituted pyrimidine scaffold. Some of these compounds possess potent anti-staphylococcal properties and potent antibacterial activities against clinically isolated MRSA strains. Compounds have been identified to exhibit low spontaneous frequency of resistance, low toxicity as well as the ability to rescuelarvae infected with lethal dose of the MRSA ATCC 43300 strain. Characterization by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purifiedFtsZ protein verified the interaction of 2,4,6-trisubstituted pyrimidine with the FtsZ protein, further confirmed by observations of iconic filamentous cell phenotype and mislocalization of the Z-ring formation. Taken together, these pyrimidine derivatives have the potential as effective treatment of staphylococcal infections.