Search results for "Pyrazolopyrimidine"

showing 2 items of 2 documents

Hsp60 Inhibitors and Modulators

2019

In this chapter, we focus on the 60 KDa Heat Shock Protein (Hsp60) and discuss some of its biological, molecular and pathological features. The structural and mechanistic aspect of the Hsp60 folding cycle will be also presented. We further illustrate how Hsp60 may be involved in many diseases and therefore considered as an effective therapeutic or theranostic target. Finally, the state-of-the-art on the development of Hsp60 and bacterial GroEL inhibitors and modulators of their expression will be illustrated. This is discussed in the light of a negative chaperonotherapy, and the consequent development of inhibitors, as well as positive chaperonotherapy, in the event its excessive activity i…

Cpn60Excessive activityHsp60 inhibitoranimal structuresHeat shock proteinChemistryPyrazolopyrimidinefungiAvrainvillamidechemical and pharmacologic phenomenaComputational biologyMizoribineSettore CHIM/06 - Chimica OrganicaCarboranylphenoxyacetanilideHsp60complex mixturesGroELGroELHspD1Heat shock proteinHSP60AvrainvillamideEpolactaene
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6-Dimethylamino 1H-pyrazolo[3,4-d]pyrimidine derivatives as new inhibitors of inflammatory mediators in intact cells.

2003

The synthesis of 6-dimethylamino 1H-pyrazolo[3,4-d]pyrimidines substituted at positions 1 and 4, and their effects on murine macrophage and human neutrophil functions are described. Several compounds and especially 4b-6b are potent inhibitors of PGE2 generation in murine macrophages. This action is related to a direct effect on COX-2 activity without affecting the enzyme expression. Some of these compounds also inhibited COX-1 and COX-2 in human monocytes and 4b showed selectivity for COX-2 inhibition. © 2003 Elsevier Science Ltd. All rights reserved.

LipopolysaccharidesMagnetic Resonance SpectroscopyPyrimidineClinical BiochemistryBlotting WesternPharmaceutical ScienceBiochemistryLeukotriene B4Pyrazolopyrimidinechemistry.chemical_compoundMiceStructure-Activity RelationshipDrug DiscoverymedicineLeukocytesMacrophageAnimalsHumansCyclooxygenase InhibitorsMolecular Biologychemistry.chemical_classificationbiologyCyclooxygenase 2 InhibitorsPancreatic ElastaseMonocyteOrganic ChemistryMembrane ProteinsBiological activityIn vitroIsoenzymesEnzymemedicine.anatomical_structurePyrimidineschemistryBiochemistryEnzyme inhibitorCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesLuminescent Measurementsbiology.proteinCyclooxygenase 1Macrophages PeritonealMolecular MedicinePyrazolesInflammation MediatorsBioorganicmedicinal chemistry
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