FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2201557068> ?p ?o ?g. }

• W2201557068 endingPage "9195" @default.
• W2201557068 startingPage "9179" @default.
• W2201557068 abstract "Our structure–activity relationship studies with N6-(2-(4-(1H-indol-5-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine derivatives led to development of a lead compound (−)-21a which exhibited very high affinity (Ki, D2 = 16.4 nM, D3 = 1.15 nM) and full agonist activity (EC50 (GTPγS); D2 = 3.23 and D3 = 1.41 nM) at both D2 and D3 receptors. A partial agonist molecule (−)-34 (EC50 (GTPγS); D2 = 21.6 (Emax = 27%) and D3 = 10.9 nM) was also identified. In a Parkinson’s disease (PD) animal model, (−)-21a was highly efficacious in reversing hypolocomotion in reserpinized rats with a long duration of action, indicating its potential as an anti-PD drug. Compound (−)-34 was also able to elevate locomotor activity in the above PD animal model significantly, implying its potential application in PD therapy. Furthermore, (−)-21a was shown to be neuroprotective in protecting neuronal PC12 from toxicity of 6-OHDA. This report, therefore, underpins the notion that a multifunctional drug like (−)-21a might have the potential not only to ameliorate motor dysfunction in PD patients but also to modify disease progression by protecting DA neurons from progressive degeneration." @default.
• W2201557068 created "2016-06-24" @default.
• W2201557068 creator A5020951431 @default.
• W2201557068 creator A5053217432 @default.
• W2201557068 creator A5060578691 @default.
• W2201557068 creator A5067129670 @default.
• W2201557068 creator A5071028108 @default.
• W2201557068 creator A5056748606 @default.
• W2201557068 date "2015-11-30" @default.
• W2201557068 modified "2023-10-10" @default.
• W2201557068 title "Development of a Highly Potent D₂/D₃ Agonist and a Partial Agonist from Structure–Activity Relationship Study of <i>N</i>⁶-(2-(4-(1<i>H</i>-Indol-5-yl)piperazin-1-yl)ethyl)-<i>N</i>⁶-propyl-4,5,6,7-tetrahydrobenzo[<i>d</i>]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson’s Disease" @default.
• W2201557068 cites W1527671059 @default.
• W2201557068 cites W1542569132 @default.
• W2201557068 cites W1971389338 @default.
• W2201557068 cites W1972789013 @default.
• W2201557068 cites W1973586027 @default.
• W2201557068 cites W1981775239 @default.
• W2201557068 cites W1990450584 @default.
• W2201557068 cites W1991241547 @default.
• W2201557068 cites W1992688100 @default.
• W2201557068 cites W2001747721 @default.
• W2201557068 cites W2002917813 @default.
• W2201557068 cites W2004575181 @default.
• W2201557068 cites W2007930722 @default.
• W2201557068 cites W2008827081 @default.
• W2201557068 cites W2011025180 @default.
• W2201557068 cites W2016693691 @default.
• W2201557068 cites W2017255858 @default.
• W2201557068 cites W2019019227 @default.
• W2201557068 cites W2019373269 @default.
• W2201557068 cites W2023158322 @default.
• W2201557068 cites W2024768658 @default.
• W2201557068 cites W2024966845 @default.
• W2201557068 cites W2030876064 @default.
• W2201557068 cites W2031740174 @default.
• W2201557068 cites W2032381724 @default.
• W2201557068 cites W2034195971 @default.
• W2201557068 cites W2039396887 @default.
• W2201557068 cites W2043209972 @default.
• W2201557068 cites W2048897966 @default.
• W2201557068 cites W2051401670 @default.
• W2201557068 cites W2053158360 @default.
• W2201557068 cites W2054631931 @default.
• W2201557068 cites W2054701937 @default.
• W2201557068 cites W2057622183 @default.
• W2201557068 cites W2062781235 @default.
• W2201557068 cites W2066354419 @default.
• W2201557068 cites W2070357349 @default.
• W2201557068 cites W2076281963 @default.
• W2201557068 cites W2077152493 @default.
• W2201557068 cites W2080673559 @default.
• W2201557068 cites W2084701770 @default.
• W2201557068 cites W2085307219 @default.
• W2201557068 cites W2085518524 @default.
• W2201557068 cites W2086612346 @default.
• W2201557068 cites W2086709975 @default.
• W2201557068 cites W2086857730 @default.
• W2201557068 cites W2087848764 @default.
• W2201557068 cites W2088136853 @default.
• W2201557068 cites W2089320827 @default.
• W2201557068 cites W2096219000 @default.
• W2201557068 cites W2096814350 @default.
• W2201557068 cites W2097744565 @default.
• W2201557068 cites W2109481524 @default.
• W2201557068 cites W2122564376 @default.
• W2201557068 cites W2122995608 @default.
• W2201557068 cites W2143959688 @default.
• W2201557068 cites W2160622942 @default.
• W2201557068 cites W2166217068 @default.
• W2201557068 cites W2167497731 @default.
• W2201557068 cites W2320246526 @default.
• W2201557068 cites W2419436028 @default.
• W2201557068 cites W4232278638 @default.
• W2201557068 doi "https://doi.org/10.1021/acs.jmedchem.5b01031" @default.
• W2201557068 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6250127" @default.
• W2201557068 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26555041" @default.
• W2201557068 hasPublicationYear "2015" @default.
• W2201557068 type Work @default.
• W2201557068 sameAs 2201557068 @default.
• W2201557068 citedByCount "36" @default.
• W2201557068 countsByYear W22015570682016 @default.
• W2201557068 countsByYear W22015570682017 @default.
• W2201557068 countsByYear W22015570682018 @default.
• W2201557068 countsByYear W22015570682019 @default.
• W2201557068 countsByYear W22015570682020 @default.
• W2201557068 countsByYear W22015570682021 @default.
• W2201557068 countsByYear W22015570682022 @default.
• W2201557068 countsByYear W22015570682023 @default.
• W2201557068 crossrefType "journal-article" @default.
• W2201557068 hasAuthorship W2201557068A5020951431 @default.
• W2201557068 hasAuthorship W2201557068A5053217432 @default.
• W2201557068 hasAuthorship W2201557068A5056748606 @default.
• W2201557068 hasAuthorship W2201557068A5060578691 @default.
• W2201557068 hasAuthorship W2201557068A5067129670 @default.
• W2201557068 hasAuthorship W2201557068A5071028108 @default.
• W2201557068 hasBestOaLocation W22015570682 @default.
• W2201557068 hasConcept C170493617 @default.
• W2201557068 hasConcept C185592680 @default.

• next