FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2006491803> ?p ?o ?g. }

• W2006491803 endingPage "356" @default.
• W2006491803 startingPage "335" @default.
• W2006491803 abstract "Three series of derivatives have been prepared by reaction of sulfanilylaminoguanidine with pyrylium salts, with the pyridinium derivatives of glycine and with the pyridinium derivatives of beta-alanine, respectively. The new compounds were assayed as inhibitors of two serine proteases, thrombin and trypsin. The study showed that in contrast to the leads, possessing KI's around 100-300 nM against thrombin, and 450-1420 nM against trypsin, respectively, the new derivatives showed inhibition constants in the range of 15-50 nM against thrombin, whereas their affinity for trypsin remained relatively low. Derivatives of beta-alanine were more active than the corresponding glycine derivatives, which in turn were more inhibitory than the pyridinium derivatives of sulfanilylaminoguanidine possessing the same substitution pattern at the pyridinium ring. Thus, the present study proposes two novel approaches for the preparation of high affinity, specific thrombin inhibitors: a novel S1 anchoring moiety in the already large family of arginine/amidine-based inhibitors, i.e., the SO2NHNHC(=NH)NH2 group, and novel non-peptidomimetic scaffolds obtained by incorporating alkyl-/aryl-substituted-pyridinium moieties in the hydrophobic binding site(s). The first one is important for obtaining bioavailable thrombin inhibitors, devoid of the high basicity of the commonly used arginine/amidine-based inhibitors, whereas the second one may lead to improved water solubility of such compounds." @default.
• W2006491803 created "2016-06-24" @default.
• W2006491803 creator A5006759876 @default.
• W2006491803 creator A5019184633 @default.
• W2006491803 creator A5035652477 @default.
• W2006491803 creator A5086011099 @default.
• W2006491803 date "2000-01-01" @default.
• W2006491803 modified "2023-09-26" @default.
• W2006491803 title "Protease Inhibitors: Part 4. Synthesis of Weakly Basic Thrombin Inhibitors Incorporating Pyridinium-Sulfanilylaminoguanidine Moieties" @default.
• W2006491803 cites W141217221 @default.
• W2006491803 cites W14547982 @default.
• W2006491803 cites W1967128898 @default.
• W2006491803 cites W1971532646 @default.
• W2006491803 cites W1971696680 @default.
• W2006491803 cites W1972768458 @default.
• W2006491803 cites W1973689793 @default.
• W2006491803 cites W1974947009 @default.
• W2006491803 cites W1975773321 @default.
• W2006491803 cites W1979904607 @default.
• W2006491803 cites W2001216966 @default.
• W2006491803 cites W2006764505 @default.
• W2006491803 cites W2014347434 @default.
• W2006491803 cites W2047710685 @default.
• W2006491803 cites W2048859138 @default.
• W2006491803 cites W2050046796 @default.
• W2006491803 cites W2063683800 @default.
• W2006491803 cites W2064643750 @default.
• W2006491803 cites W2071184125 @default.
• W2006491803 cites W2081090776 @default.
• W2006491803 cites W2085332043 @default.
• W2006491803 cites W2087522305 @default.
• W2006491803 cites W2091379422 @default.
• W2006491803 cites W2094680415 @default.
• W2006491803 cites W2096306307 @default.
• W2006491803 cites W2096373077 @default.
• W2006491803 cites W2112612483 @default.
• W2006491803 cites W2121897924 @default.
• W2006491803 cites W2181120820 @default.
• W2006491803 cites W2240180620 @default.
• W2006491803 cites W2314049493 @default.
• W2006491803 cites W2316806901 @default.
• W2006491803 cites W2950487297 @default.
• W2006491803 doi "https://doi.org/10.1080/14756360009040692" @default.
• W2006491803 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10995066" @default.
• W2006491803 hasPublicationYear "2000" @default.
• W2006491803 type Work @default.
• W2006491803 sameAs 2006491803 @default.
• W2006491803 citedByCount "2" @default.
• W2006491803 crossrefType "journal-article" @default.
• W2006491803 hasAuthorship W2006491803A5006759876 @default.
• W2006491803 hasAuthorship W2006491803A5019184633 @default.
• W2006491803 hasAuthorship W2006491803A5035652477 @default.
• W2006491803 hasAuthorship W2006491803A5086011099 @default.
• W2006491803 hasBestOaLocation W20064918031 @default.
• W2006491803 hasConcept C155647269 @default.
• W2006491803 hasConcept C181199279 @default.
• W2006491803 hasConcept C185592680 @default.
• W2006491803 hasConcept C203014093 @default.
• W2006491803 hasConcept C2776414213 @default.
• W2006491803 hasConcept C2776568683 @default.
• W2006491803 hasConcept C2776714187 @default.
• W2006491803 hasConcept C2776980637 @default.
• W2006491803 hasConcept C2777221202 @default.
• W2006491803 hasConcept C2777292125 @default.
• W2006491803 hasConcept C2777756961 @default.
• W2006491803 hasConcept C2777807008 @default.
• W2006491803 hasConcept C2778622868 @default.
• W2006491803 hasConcept C2779288520 @default.
• W2006491803 hasConcept C2780340462 @default.
• W2006491803 hasConcept C515207424 @default.
• W2006491803 hasConcept C55493867 @default.
• W2006491803 hasConcept C57002609 @default.
• W2006491803 hasConcept C71240020 @default.
• W2006491803 hasConcept C86803240 @default.
• W2006491803 hasConcept C89560881 @default.
• W2006491803 hasConceptScore W2006491803C155647269 @default.
• W2006491803 hasConceptScore W2006491803C181199279 @default.
• W2006491803 hasConceptScore W2006491803C185592680 @default.
• W2006491803 hasConceptScore W2006491803C203014093 @default.
• W2006491803 hasConceptScore W2006491803C2776414213 @default.
• W2006491803 hasConceptScore W2006491803C2776568683 @default.
• W2006491803 hasConceptScore W2006491803C2776714187 @default.
• W2006491803 hasConceptScore W2006491803C2776980637 @default.
• W2006491803 hasConceptScore W2006491803C2777221202 @default.
• W2006491803 hasConceptScore W2006491803C2777292125 @default.
• W2006491803 hasConceptScore W2006491803C2777756961 @default.
• W2006491803 hasConceptScore W2006491803C2777807008 @default.
• W2006491803 hasConceptScore W2006491803C2778622868 @default.
• W2006491803 hasConceptScore W2006491803C2779288520 @default.
• W2006491803 hasConceptScore W2006491803C2780340462 @default.
• W2006491803 hasConceptScore W2006491803C515207424 @default.
• W2006491803 hasConceptScore W2006491803C55493867 @default.
• W2006491803 hasConceptScore W2006491803C57002609 @default.
• W2006491803 hasConceptScore W2006491803C71240020 @default.
• W2006491803 hasConceptScore W2006491803C86803240 @default.
• W2006491803 hasConceptScore W2006491803C89560881 @default.
• W2006491803 hasIssue "4" @default.
• W2006491803 hasLocation W20064918031 @default.

• next