FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1966746582> ?p ?o ?g. }

• W1966746582 endingPage "2174" @default.
• W1966746582 startingPage "2163" @default.
• W1966746582 abstract "In this study, a novel series of imidazole-containing compounds with dual properties, that is, inhibitory potency at the enzyme histamine N(tau)-methyltransferase (HMT) and antagonist potency at histamine H(3) receptors was designed and synthesized. Pharmacologically, these new hybrid drugs were evaluated in functional assays for their inhibitory potencies at rat kidney HMT and for their antagonist activities on synaptosomes of rat cerebral cortex. For selected compounds, binding affinities at recombinant human histamine H(3) receptors were determined. The first compounds (1-10) of the series proved to be H(3) receptor ligands of high potency at rat synaptosomes or of high binding affinity at human H(3) receptors, respectively, but of only moderate activity as inhibitors of rat kidney HMT. In contrast, aminoquinoline- or tetrahydroacridine-containing derivatives 11-17 also displayed HMT inhibitory potency in the nanomolar concentration range. Preliminary data from molecular modeling investigations showed that the imidazole derivative 15 and the HMT inhibitor quinacrine possess identical binding areas. The most interesting compound (14) is simultaneously a highly potent H(3) receptor ligand (K(i)=4.1nM) and a highly potent HMT inhibitor (IC(50)=24nM), which makes this derivative a valuable pharmacological tool for further development." @default.
• W1966746582 created "2016-06-24" @default.
• W1966746582 creator A5007974371 @default.
• W1966746582 creator A5013795906 @default.
• W1966746582 creator A5016614839 @default.
• W1966746582 creator A5020624343 @default.
• W1966746582 creator A5022326769 @default.
• W1966746582 creator A5022345732 @default.
• W1966746582 creator A5037960139 @default.
• W1966746582 creator A5053509756 @default.
• W1966746582 creator A5055328126 @default.
• W1966746582 creator A5088794437 @default.
• W1966746582 creator A5090140984 @default.
• W1966746582 date "2003-05-01" @default.
• W1966746582 modified "2023-09-27" @default.
• W1966746582 title "Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine hH3 receptor affinities" @default.
• W1966746582 cites W1672160734 @default.
• W1966746582 cites W1961819790 @default.
• W1966746582 cites W1964403533 @default.
• W1966746582 cites W1964958542 @default.
• W1966746582 cites W1966041739 @default.
• W1966746582 cites W1967589368 @default.
• W1966746582 cites W1967843166 @default.
• W1966746582 cites W1968312067 @default.
• W1966746582 cites W1971707549 @default.
• W1966746582 cites W1973687438 @default.
• W1966746582 cites W1974845204 @default.
• W1966746582 cites W1976893442 @default.
• W1966746582 cites W1985411297 @default.
• W1966746582 cites W1988881554 @default.
• W1966746582 cites W1989846049 @default.
• W1966746582 cites W1993545839 @default.
• W1966746582 cites W1994376303 @default.
• W1966746582 cites W1998488929 @default.
• W1966746582 cites W2001079294 @default.
• W1966746582 cites W2001945805 @default.
• W1966746582 cites W2008636145 @default.
• W1966746582 cites W2039031830 @default.
• W1966746582 cites W2043391766 @default.
• W1966746582 cites W2046546985 @default.
• W1966746582 cites W2046653273 @default.
• W1966746582 cites W2046696965 @default.
• W1966746582 cites W2065448466 @default.
• W1966746582 cites W2071962985 @default.
• W1966746582 cites W2074631079 @default.
• W1966746582 cites W2077687762 @default.
• W1966746582 cites W2091662140 @default.
• W1966746582 cites W2093157257 @default.
• W1966746582 cites W2093809581 @default.
• W1966746582 cites W2094605937 @default.
• W1966746582 cites W2098568143 @default.
• W1966746582 cites W2102773142 @default.
• W1966746582 cites W2114808045 @default.
• W1966746582 cites W2155524113 @default.
• W1966746582 cites W2156259759 @default.
• W1966746582 cites W2157165549 @default.
• W1966746582 cites W2329783263 @default.
• W1966746582 cites W233628489 @default.
• W1966746582 cites W2490970362 @default.
• W1966746582 cites W4245658862 @default.
• W1966746582 doi "https://doi.org/10.1016/s0968-0896(03)00120-2" @default.
• W1966746582 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12713826" @default.
• W1966746582 hasPublicationYear "2003" @default.
• W1966746582 type Work @default.
• W1966746582 sameAs 1966746582 @default.
• W1966746582 citedByCount "28" @default.
• W1966746582 countsByYear W19667465822012 @default.
• W1966746582 countsByYear W19667465822013 @default.
• W1966746582 countsByYear W19667465822014 @default.
• W1966746582 countsByYear W19667465822015 @default.
• W1966746582 countsByYear W19667465822016 @default.
• W1966746582 countsByYear W19667465822019 @default.
• W1966746582 countsByYear W19667465822021 @default.
• W1966746582 crossrefType "journal-article" @default.
• W1966746582 hasAuthorship W1966746582A5007974371 @default.
• W1966746582 hasAuthorship W1966746582A5013795906 @default.
• W1966746582 hasAuthorship W1966746582A5016614839 @default.
• W1966746582 hasAuthorship W1966746582A5020624343 @default.
• W1966746582 hasAuthorship W1966746582A5022326769 @default.
• W1966746582 hasAuthorship W1966746582A5022345732 @default.
• W1966746582 hasAuthorship W1966746582A5037960139 @default.
• W1966746582 hasAuthorship W1966746582A5053509756 @default.
• W1966746582 hasAuthorship W1966746582A5055328126 @default.
• W1966746582 hasAuthorship W1966746582A5088794437 @default.
• W1966746582 hasAuthorship W1966746582A5090140984 @default.
• W1966746582 hasConcept C1122143 @default.
• W1966746582 hasConcept C116569031 @default.
• W1966746582 hasConcept C159545944 @default.
• W1966746582 hasConcept C170493617 @default.
• W1966746582 hasConcept C185592680 @default.
• W1966746582 hasConcept C187507357 @default.
• W1966746582 hasConcept C202751555 @default.
• W1966746582 hasConcept C2776885963 @default.
• W1966746582 hasConcept C2780283098 @default.
• W1966746582 hasConcept C2780874372 @default.
• W1966746582 hasConcept C34400551 @default.
• W1966746582 hasConcept C55493867 @default.
• W1966746582 hasConcept C57992300 @default.

• next