http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-114634506-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d4822dfff5709a719ddfb821a88a04d7 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-04 |
| filingDate | 2022-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4209d4734d1445d1cbab12daf52af059 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61ba0252dd69619a6ead211afd183e77 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c190fdc43381d1254897e640270c7816 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_884f3aca173480e650a62f09b6510f61 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7932c237c86a9bb4fda09538dc817c15 |
| publicationDate | 2022-06-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-114634506-A |
| titleOfInvention | Substituted 1H-indol-2-one-linked-3,5-substituted aryl-1,3-thiazolidinone derivatives |
| abstract | The invention belongs to the technical field of medicine, and particularly relates to a substituted 1H-indol-2-ketone-link-3,5-substituted aryl-substituted-1,3-thiazolidinone derivative and a preparation method and application thereof. The invention adopts computer-aided drug design technology, and on the basis of analyzing the three-dimensional structure of PTP1B protein, aiming at the active site of PTP1B, 1H-indol-2-ketone and thiazolidine-4-ketone fragments with extensive biological activities are selected as the structural core. , using the piecing principle to design and synthesize a series of PTP1B small molecule inhibitors with 1H-indol-2-ketone-linking-3,5-substituted aryl-1,3-thiazolidine-4-ketone basic skeleton. The PTP1B enzyme inhibitory activity test showed that the compounds showed good PTP1B inhibitory activity at a concentration of 5μg/mL, and the inhibition rate was more than 50%; the IC 50 value was between 0.89 and 12.60μM. Molecular docking showed that the target compound interacted well with multiple action sites of the enzyme. The present invention provides theoretical basis and material basis for developing novel PTP1B inhibitors. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2023160708-A1 |
| priorityDate | 2022-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 109.