FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1978245422> ?p ?o ?g. }

• W1978245422 endingPage "5950" @default.
• W1978245422 startingPage "5942" @default.
• W1978245422 abstract "Urea transporters, which include UT-B in kidney microvessels, are potential targets for development of drugs with a novel diuretic (‘urearetic’) mechanism. We recently identified, by high-throughput screening, a triazolothienopyrimidine UT-B inhibitor, 1, that selectively and reversibly inhibited urea transport with IC50 = 25.1 nM and reduced urinary concentration in mice (Yao et al.J. Am. Soc. Nephrol., in press). Here, we analyzed 273 commercially available analogues of 1 to establish a structure–activity series and synthesized a targeted library of 11 analogues to identify potent, metabolically stable UT-B inhibitors. The best compound, {3-[4-(1,1-difluoroethyl)benzenesulfonyl]thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-yl}thiophen-2-ylmethylamine, 3k, had IC50 of 23 and 15 nM for inhibition of urea transport by mouse and human UT-B, respectively, and ∼40-fold improved in vitro metabolic stability compared to 1. In mice, 3k accumulated in kidney and urine and reduced maximum urinary concentration. Triazolothienopyrimidines may be useful for therapy of diuretic-refractory edema in heart and liver failure." @default.
• W1978245422 created "2016-06-24" @default.
• W1978245422 creator A5007292193 @default.
• W1978245422 creator A5021293751 @default.
• W1978245422 creator A5025355667 @default.
• W1978245422 creator A5037051366 @default.
• W1978245422 creator A5042356327 @default.
• W1978245422 creator A5063772512 @default.
• W1978245422 date "2012-06-19" @default.
• W1978245422 modified "2023-10-18" @default.
• W1978245422 title "Nanomolar Potency and Metabolically Stable Inhibitors of Kidney Urea Transporter UT-B" @default.
• W1978245422 cites W1586241840 @default.
• W1978245422 cites W1986543162 @default.
• W1978245422 cites W1992439000 @default.
• W1978245422 cites W1999664492 @default.
• W1978245422 cites W2013480765 @default.
• W1978245422 cites W2050400976 @default.
• W1978245422 cites W2056381596 @default.
• W1978245422 cites W2056703832 @default.
• W1978245422 cites W2063549176 @default.
• W1978245422 cites W2071050259 @default.
• W1978245422 cites W2073257976 @default.
• W1978245422 cites W2080823491 @default.
• W1978245422 cites W2081397360 @default.
• W1978245422 cites W2096574170 @default.
• W1978245422 cites W2144009346 @default.
• W1978245422 cites W2145909643 @default.
• W1978245422 cites W2145910029 @default.
• W1978245422 cites W2145958552 @default.
• W1978245422 cites W2148470566 @default.
• W1978245422 cites W2154542182 @default.
• W1978245422 cites W2161354173 @default.
• W1978245422 cites W2949511477 @default.
• W1978245422 cites W4231644331 @default.
• W1978245422 doi "https://doi.org/10.1021/jm300491y" @default.
• W1978245422 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3590912" @default.
• W1978245422 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22694147" @default.
• W1978245422 hasPublicationYear "2012" @default.
• W1978245422 type Work @default.
• W1978245422 sameAs 1978245422 @default.
• W1978245422 citedByCount "110" @default.
• W1978245422 countsByYear W19782454222012 @default.
• W1978245422 countsByYear W19782454222013 @default.
• W1978245422 countsByYear W19782454222014 @default.
• W1978245422 countsByYear W19782454222015 @default.
• W1978245422 countsByYear W19782454222016 @default.
• W1978245422 countsByYear W19782454222017 @default.
• W1978245422 countsByYear W19782454222018 @default.
• W1978245422 countsByYear W19782454222019 @default.
• W1978245422 countsByYear W19782454222020 @default.
• W1978245422 countsByYear W19782454222021 @default.
• W1978245422 countsByYear W19782454222022 @default.
• W1978245422 countsByYear W19782454222023 @default.
• W1978245422 crossrefType "journal-article" @default.
• W1978245422 hasAuthorship W1978245422A5007292193 @default.
• W1978245422 hasAuthorship W1978245422A5021293751 @default.
• W1978245422 hasAuthorship W1978245422A5025355667 @default.
• W1978245422 hasAuthorship W1978245422A5037051366 @default.
• W1978245422 hasAuthorship W1978245422A5042356327 @default.
• W1978245422 hasAuthorship W1978245422A5063772512 @default.
• W1978245422 hasBestOaLocation W19782454222 @default.
• W1978245422 hasConcept C104317684 @default.
• W1978245422 hasConcept C134018914 @default.
• W1978245422 hasConcept C149011108 @default.
• W1978245422 hasConcept C185592680 @default.
• W1978245422 hasConcept C202751555 @default.
• W1978245422 hasConcept C2777752497 @default.
• W1978245422 hasConcept C2779918671 @default.
• W1978245422 hasConcept C2780091579 @default.
• W1978245422 hasConcept C2780365088 @default.
• W1978245422 hasConcept C55493867 @default.
• W1978245422 hasConcept C57992300 @default.
• W1978245422 hasConcept C71924100 @default.
• W1978245422 hasConcept C98274493 @default.
• W1978245422 hasConceptScore W1978245422C104317684 @default.
• W1978245422 hasConceptScore W1978245422C134018914 @default.
• W1978245422 hasConceptScore W1978245422C149011108 @default.
• W1978245422 hasConceptScore W1978245422C185592680 @default.
• W1978245422 hasConceptScore W1978245422C202751555 @default.
• W1978245422 hasConceptScore W1978245422C2777752497 @default.
• W1978245422 hasConceptScore W1978245422C2779918671 @default.
• W1978245422 hasConceptScore W1978245422C2780091579 @default.
• W1978245422 hasConceptScore W1978245422C2780365088 @default.
• W1978245422 hasConceptScore W1978245422C55493867 @default.
• W1978245422 hasConceptScore W1978245422C57992300 @default.
• W1978245422 hasConceptScore W1978245422C71924100 @default.
• W1978245422 hasConceptScore W1978245422C98274493 @default.
• W1978245422 hasIssue "12" @default.
• W1978245422 hasLocation W19782454221 @default.
• W1978245422 hasLocation W19782454222 @default.
• W1978245422 hasLocation W19782454223 @default.
• W1978245422 hasLocation W19782454224 @default.
• W1978245422 hasLocation W19782454225 @default.
• W1978245422 hasOpenAccess W1978245422 @default.
• W1978245422 hasPrimaryLocation W19782454221 @default.
• W1978245422 hasRelatedWork W1033667931 @default.
• W1978245422 hasRelatedWork W1978245422 @default.
• W1978245422 hasRelatedWork W2171273833 @default.

• next