http://rdf.ncbi.nlm.nih.gov/pubchem/patent/MX-2012014556-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_fe3f2d4f405df889e4d23b14700ba764 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-00 |
| filingDate | 2012-12-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5a25874f9befde75037b0b7c54f84d2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1b6c0089713cfbce00861079982e9deb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fccec0f17a72f855d046cc9696355112 |
| publicationDate | 2014-06-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | MX-2012014556-A |
| titleOfInvention | DERIVATIVES OF 6-QUINOXALINAMINE AS INHIBITORS OF THE INFLUENZA A VIRUS NEURAMINIDASE (H1N1). |
| abstract | The present invention has as main objective to find new inhibitors directed against hemagglutinin (HA) and neuraminidase (NA) of influenza A virus (H1N1), based on the search for fragments. The present invention relates to compounds in the biotechnological field that have antiviral activity, particularly against influenza AHIN1. Based on the principles of drug design by fragment search, the Maybridge Ro3 library of 1000 chemical fragments was screened, evaluating the effect of the compounds on the HA and NA of the human influenza virus. Recombinant neuraminidase was incubated with the compounds and the inhibition of enzyme activity was estimated, detecting the fluorescent product of the reaction, where HA screening was performed by determining the inhibition of hemagglutinating activity of influenza virus when incubated with the compounds The influenza A (H1N1) Mexico / 2009 virus used in the trials was produced in MDCK cells growing on microacarrines in suspension in serum-free medium. Five HA inhibitor compounds and 13 NA inhibitor compounds were found. The compound 1-azepanil (3-piperidinyl) methanone (AzPM) and the compound 6-aminoquinozalina (AQA), with activity on NA were studied in depth. The identity of and purity of the AzPM compound was confirmed by 13C NMR. The AzPM compound was confirmed as a recombinant NA inhibitor. Likewise, it was found that the inhibition of NA by AzPM decreases in the presence of calcium, since it is involved in maintaining the thermal stability and quaternary structure of NA. The 95% AQA compound was confirmed as an inhibitor of NA in the context of influenza A virus (HIN1.). |
| priorityDate | 2012-12-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 201.