http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2017291887-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_e2d694ea9a702cffaedf9ba06773948d http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dd656439ab15d45443c6dc65a2ca298f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 |
| filingDate | 2016-09-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d26dfe92274ec949111db0c42d14f00c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_70732c0e0069ce997697b4a4349cc8e5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_15b372e5070e0a0f9b4e7c328e4cdf2e |
| publicationDate | 2017-10-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-2017291887-A1 |
| titleOfInvention | Pyrimidines for treatment of bacterial infections |
| 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 rescue G. mellonella larvae infected with lethal dose of the MRSA ATCC 43300 strain. Characterization by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purified S. aureus FtsZ 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. |
| priorityDate | 2016-04-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 262.