Matches in SemOpenAlex for { <https://semopenalex.org/work/W2012197966> ?p ?o ?g. }
Showing items 1 to 84 of
84
with 100 items per page.
- W2012197966 endingPage "2020" @default.
- W2012197966 startingPage "2007" @default.
- W2012197966 abstract "A series of 4-(aminoethoxy)indoles 7 and a related series of 4-(aminoethoxy)indolones 8 were synthesized and evaluated for their affinity for both the high- and low-affinity agonist states (D2High and D2Low, respectively) of the dopamine (DA) D2 receptor. The 4-aminoethoxy derivatives (i.e., 7 and 8) were designed as bioisosteric analogues based on the phenol prototype 4. The indolones 8 were observed to have high affinity for the D2High receptor. Comparison of their previously reported chroman analogues with the more flexible 4-(aminoethoxy)indoles revealed the chroman analogues to be more potent, whereas little loss in D2High affinity was observed when comparing the 4-(aminoethoxy)indolones with their respective chroman analogues. Several regions of the phenoxyethylamine framework were modified and recognized as potential sites to modulate the level of intrinsic activity. A conformational analysis was performed and a putative bioactive conformation was proposed which fulfilled the D2 agonist pharmacophore criteria based on the McDermed model. Structure−activity relationships gained from these studies have aided in the synthesis of D2 partial agonists of varying intrinsic activity levels. These agents should be of therapeutic value in treating disorders resulting from hypo- and hyperdopaminergic activity, without the side effects associated with complete D2 agonism or antagonism." @default.
- W2012197966 created "2016-06-24" @default.
- W2012197966 creator A5001816604 @default.
- W2012197966 creator A5005166693 @default.
- W2012197966 creator A5011184273 @default.
- W2012197966 creator A5011753745 @default.
- W2012197966 creator A5028117769 @default.
- W2012197966 creator A5029909734 @default.
- W2012197966 creator A5051379328 @default.
- W2012197966 creator A5067944628 @default.
- W2012197966 creator A5074614370 @default.
- W2012197966 date "1999-05-07" @default.
- W2012197966 modified "2023-10-03" @default.
- W2012197966 title "New Generation Dopaminergic Agents. 6. Structure−Activity Relationship Studies of a Series of 4-(Aminoethoxy)indole and 4-(Aminoethoxy)indolone Derivatives Based on the Newly Discovered 3-Hydroxyphenoxyethylamine D<sub>2</sub> Template" @default.
- W2012197966 cites W135975038 @default.
- W2012197966 cites W1965599562 @default.
- W2012197966 cites W2002159489 @default.
- W2012197966 cites W2003784342 @default.
- W2012197966 cites W2015612733 @default.
- W2012197966 cites W2068064905 @default.
- W2012197966 cites W2099793114 @default.
- W2012197966 cites W2162774153 @default.
- W2012197966 doi "https://doi.org/10.1021/jm990023s" @default.
- W2012197966 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10354409" @default.
- W2012197966 hasPublicationYear "1999" @default.
- W2012197966 type Work @default.
- W2012197966 sameAs 2012197966 @default.
- W2012197966 citedByCount "14" @default.
- W2012197966 countsByYear W20121979662014 @default.
- W2012197966 countsByYear W20121979662017 @default.
- W2012197966 countsByYear W20121979662019 @default.
- W2012197966 countsByYear W20121979662020 @default.
- W2012197966 crossrefType "journal-article" @default.
- W2012197966 hasAuthorship W2012197966A5001816604 @default.
- W2012197966 hasAuthorship W2012197966A5005166693 @default.
- W2012197966 hasAuthorship W2012197966A5011184273 @default.
- W2012197966 hasAuthorship W2012197966A5011753745 @default.
- W2012197966 hasAuthorship W2012197966A5028117769 @default.
- W2012197966 hasAuthorship W2012197966A5029909734 @default.
- W2012197966 hasAuthorship W2012197966A5051379328 @default.
- W2012197966 hasAuthorship W2012197966A5067944628 @default.
- W2012197966 hasAuthorship W2012197966A5074614370 @default.
- W2012197966 hasConcept C170493617 @default.
- W2012197966 hasConcept C185592680 @default.
- W2012197966 hasConcept C192527728 @default.
- W2012197966 hasConcept C193042331 @default.
- W2012197966 hasConcept C202751555 @default.
- W2012197966 hasConcept C2778938600 @default.
- W2012197966 hasConcept C55493867 @default.
- W2012197966 hasConcept C56173144 @default.
- W2012197966 hasConcept C58732023 @default.
- W2012197966 hasConcept C71240020 @default.
- W2012197966 hasConceptScore W2012197966C170493617 @default.
- W2012197966 hasConceptScore W2012197966C185592680 @default.
- W2012197966 hasConceptScore W2012197966C192527728 @default.
- W2012197966 hasConceptScore W2012197966C193042331 @default.
- W2012197966 hasConceptScore W2012197966C202751555 @default.
- W2012197966 hasConceptScore W2012197966C2778938600 @default.
- W2012197966 hasConceptScore W2012197966C55493867 @default.
- W2012197966 hasConceptScore W2012197966C56173144 @default.
- W2012197966 hasConceptScore W2012197966C58732023 @default.
- W2012197966 hasConceptScore W2012197966C71240020 @default.
- W2012197966 hasIssue "11" @default.
- W2012197966 hasLocation W20121979661 @default.
- W2012197966 hasLocation W20121979662 @default.
- W2012197966 hasOpenAccess W2012197966 @default.
- W2012197966 hasPrimaryLocation W20121979661 @default.
- W2012197966 hasRelatedWork W1574889367 @default.
- W2012197966 hasRelatedWork W1975860867 @default.
- W2012197966 hasRelatedWork W1996675005 @default.
- W2012197966 hasRelatedWork W2024469040 @default.
- W2012197966 hasRelatedWork W2045229648 @default.
- W2012197966 hasRelatedWork W2083839784 @default.
- W2012197966 hasRelatedWork W2091806755 @default.
- W2012197966 hasRelatedWork W2949794922 @default.
- W2012197966 hasRelatedWork W2951110508 @default.
- W2012197966 hasRelatedWork W3016695804 @default.
- W2012197966 hasVolume "42" @default.
- W2012197966 isParatext "false" @default.
- W2012197966 isRetracted "false" @default.
- W2012197966 magId "2012197966" @default.
- W2012197966 workType "article" @default.