FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2042157018> ?p ?o ?g. }

• W2042157018 endingPage "14202" @default.
• W2042157018 startingPage "14186" @default.
• W2042157018 abstract "Premedication with a combination of histamine H₁ receptor (H₁R) and H₂ receptor (H₂R) antagonists has been suggested as a prophylactic principle, for instance, in anaesthesia and surgery. Aiming at pharmacological hybrids combining H₁R and H₂R antagonistic activity, a series of cyanoguanidines 14-35 was synthesized by linking mepyramine-type H₁R antagonist substructures with roxatidine-, tiotidine-, or ranitidine-type H₂R antagonist moieties. N-desmethylmepyramine was connected via a poly-methylene spacer to a cyanoguanidine group as the urea equivalent of the H₂R antagonist moiety. The title compounds were screened for histamine antagonistic activity at the isolated ileum (H₁R) and the isolated spontaneously beating right atrium (H₂R) of the guinea pig. The results indicate that, depending on the nature of the H₂R antagonist partial structure, the highest H₁R antagonist potency resided in roxatidine-type compounds with spacers of six methylene groups in length (compound 21), and tiotidine-type compounds irrespective of the alkyl chain length (compounds 28, 32, 33), N-cyano-N'-[2-[[(2-guanidino-4-thiazolyl)methyl]thio]ethyl]-N″-[2-[N-[2-[N-(4-methoxybenzyl)-N-(pyridyl)-amino] ethyl]-N-methylamino]ethyl] guanidine (25, pKB values: 8.05 (H₁R, ileum) and 7.73 (H₂R, atrium) and the homologue with the mepyramine moiety connected by a six-membered chain to the tiotidine-like partial structure (compound 32, pKB values: 8.61 (H₁R) and 6.61 (H₂R) were among the most potent hybrid compounds. With respect to the development of a potential pharmacotherapeutic agent, structural optimization seems possible through selection of other H₁R and H₂R pharmacophoric moieties with mutually affinity-enhancing properties." @default.
• W2042157018 created "2016-06-24" @default.
• W2042157018 creator A5007797524 @default.
• W2042157018 creator A5028661610 @default.
• W2042157018 creator A5034401167 @default.
• W2042157018 creator A5076810446 @default.
• W2042157018 date "2013-11-15" @default.
• W2042157018 modified "2023-10-06" @default.
• W2042157018 title "Synthesis and Dual Histamine H1 and H2 Receptor Antagonist Activity of Cyanoguanidine Derivatives" @default.
• W2042157018 cites W122033644 @default.
• W2042157018 cites W1971934044 @default.
• W2042157018 cites W1996486246 @default.
• W2042157018 cites W2002641744 @default.
• W2042157018 cites W2006912125 @default.
• W2042157018 cites W2026694261 @default.
• W2042157018 cites W2053826416 @default.
• W2042157018 cites W2056521778 @default.
• W2042157018 cites W2067911789 @default.
• W2042157018 cites W2068293422 @default.
• W2042157018 cites W2074949244 @default.
• W2042157018 cites W2083551870 @default.
• W2042157018 cites W2084028147 @default.
• W2042157018 cites W2102982141 @default.
• W2042157018 cites W2124325125 @default.
• W2042157018 cites W2124685011 @default.
• W2042157018 cites W2143183230 @default.
• W2042157018 cites W2152082300 @default.
• W2042157018 cites W2160522866 @default.
• W2042157018 cites W2162570207 @default.
• W2042157018 cites W2168637564 @default.
• W2042157018 cites W2316169215 @default.
• W2042157018 cites W2352784539 @default.
• W2042157018 cites W2396463931 @default.
• W2042157018 cites W267004816 @default.
• W2042157018 cites W2951742105 @default.
• W2042157018 doi "https://doi.org/10.3390/molecules181114186" @default.
• W2042157018 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6269795" @default.
• W2042157018 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24248146" @default.
• W2042157018 hasPublicationYear "2013" @default.
• W2042157018 type Work @default.
• W2042157018 sameAs 2042157018 @default.
• W2042157018 citedByCount "10" @default.
• W2042157018 countsByYear W20421570182014 @default.
• W2042157018 countsByYear W20421570182015 @default.
• W2042157018 countsByYear W20421570182016 @default.
• W2042157018 countsByYear W20421570182017 @default.
• W2042157018 countsByYear W20421570182019 @default.
• W2042157018 countsByYear W20421570182022 @default.
• W2042157018 crossrefType "journal-article" @default.
• W2042157018 hasAuthorship W2042157018A5007797524 @default.
• W2042157018 hasAuthorship W2042157018A5028661610 @default.
• W2042157018 hasAuthorship W2042157018A5034401167 @default.
• W2042157018 hasAuthorship W2042157018A5076810446 @default.
• W2042157018 hasBestOaLocation W20421570181 @default.
• W2042157018 hasConcept C1122143 @default.
• W2042157018 hasConcept C170493617 @default.
• W2042157018 hasConcept C185592680 @default.
• W2042157018 hasConcept C2776568683 @default.
• W2042157018 hasConcept C2776885963 @default.
• W2042157018 hasConcept C2779090179 @default.
• W2042157018 hasConcept C2779463914 @default.
• W2042157018 hasConcept C2780719153 @default.
• W2042157018 hasConcept C2781253882 @default.
• W2042157018 hasConcept C55493867 @default.
• W2042157018 hasConcept C71240020 @default.
• W2042157018 hasConcept C86803240 @default.
• W2042157018 hasConcept C98274493 @default.
• W2042157018 hasConceptScore W2042157018C1122143 @default.
• W2042157018 hasConceptScore W2042157018C170493617 @default.
• W2042157018 hasConceptScore W2042157018C185592680 @default.
• W2042157018 hasConceptScore W2042157018C2776568683 @default.
• W2042157018 hasConceptScore W2042157018C2776885963 @default.
• W2042157018 hasConceptScore W2042157018C2779090179 @default.
• W2042157018 hasConceptScore W2042157018C2779463914 @default.
• W2042157018 hasConceptScore W2042157018C2780719153 @default.
• W2042157018 hasConceptScore W2042157018C2781253882 @default.
• W2042157018 hasConceptScore W2042157018C55493867 @default.
• W2042157018 hasConceptScore W2042157018C71240020 @default.
• W2042157018 hasConceptScore W2042157018C86803240 @default.
• W2042157018 hasConceptScore W2042157018C98274493 @default.
• W2042157018 hasIssue "11" @default.
• W2042157018 hasLocation W20421570181 @default.
• W2042157018 hasLocation W20421570182 @default.
• W2042157018 hasLocation W20421570183 @default.
• W2042157018 hasLocation W20421570184 @default.
• W2042157018 hasLocation W20421570185 @default.
• W2042157018 hasLocation W20421570186 @default.
• W2042157018 hasOpenAccess W2042157018 @default.
• W2042157018 hasPrimaryLocation W20421570181 @default.
• W2042157018 hasRelatedWork W1992526122 @default.
• W2042157018 hasRelatedWork W2005180775 @default.
• W2042157018 hasRelatedWork W2041509453 @default.
• W2042157018 hasRelatedWork W2045060966 @default.
• W2042157018 hasRelatedWork W2046299183 @default.
• W2042157018 hasRelatedWork W2078461625 @default.
• W2042157018 hasRelatedWork W2118595345 @default.
• W2042157018 hasRelatedWork W2161333028 @default.
• W2042157018 hasRelatedWork W2472127694 @default.

• next