http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010045510-A2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5827520702f36e107e4c3d93914ce697 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f20e49ad9b366a771ab0adc4fa022004 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f4d33b034f16ba7d618cfa223acaea8f http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_46ec2ebcf0f0bc6876db446e70f8ba64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3f3bb47869bd4af2afdccca8264b1b85 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G16C20-40 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G16C20-50 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-16 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/G06F19-16 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/G06F19-00 |
| filingDate | 2009-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d5ccd0b2a1a0a49467de356ca166040e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a8c7d391c28784c5c5e5eb805b16998 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_99d04cf042d594606a655f194fa116ec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd66a2b0f7c7bf758ea67351e7e4f6f5 |
| publicationDate | 2010-04-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | WO-2010045510-A2 |
| titleOfInvention | A model for glutamate racemase inhibitors and glutamate racemase antibacterial agents |
| abstract | The increase in antibacterial resistance has created the demand for new antibiotics. The present invention relates to a more potent antibiotic that targets the enzyme glutamate racemase from known glutamate racemase inhibitors. Glutamate racemase catalyses the interconversion of L-glutamate to D-glutamate, making D-glutamate available, which is required for bacterial peptidoglycan biosynthesis. Knockout mutations have shown glutamate racemase to be necessary for bacterial cell survival and, before the present invention, no antibiotic on the market targeted this enzyme. The present invention relates to new, ligand based glutamate racemase inhibitors, developed using software to extract a pharmacophore model from a group of known glutamate racemase inhibitors. Forty-seven (47) known inhibitors were collected from the literature and several pharmacophore models were extracted therefrom. The functional groups common to all the known inhibitors were included in a pharmacophore model that described the requirements for glutamate racemase inhibition with 82% accuracy. Of these models, one was found to describe the requirements for glutamate racemase inhibition with 82% accuracy. The model was used to search databases of commercially available chemical compounds and 2-(2-(l/i-indol-3-yl)ethylamino)-4-oxo-4-p-tolylbutanoic acid and 2-(2-(l//-indol-3-yl)ethylamino)-4-(4-fluorophenyl)-4-oxobutanoic acid were identified as showing antibacterial activity. These compounds were assayed against S. pneumoniae and were shown to have antibacterial activity against the non- virulent strain R6 and against a multidrug resistant strain. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110294707-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113284566-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113284566-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102184284-A |
| priorityDate | 2008-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 425.