Matches in SemOpenAlex for { <https://semopenalex.org/work/W2056464524> ?p ?o ?g. }
- W2056464524 endingPage "5041" @default.
- W2056464524 startingPage "5033" @default.
- W2056464524 abstract "Hypoglycemic agents with a mechanism of depeptidyl peptidase IV (DPP-4) inhibition are suitable for once daily oral dosing. It is difficult to strike a balance between inhibitory activity and duration of action in plasma for inhibitors bearing an electrophilic nitrile group. We explored fused bicyclic heteroarylpiperazine substituted at the γ-position of the proline structure in the investigation of l-prolylthiazolidines lacking the electrophilic nitrile. Among them, 2-trifluoroquinolyl compound 8g is the most potent, long-lasting DPP-4 inhibitor (IC50 = 0.37 nmol/L) with high selectivity against other related peptidases. X-ray crystal structure determination of 8g indicates that CH-π interactions generated between the quinolyl ring and the guanidinyl group of Arg358 enhances the DPP-4 inhibitory activity and selectivity." @default.
- W2056464524 created "2016-06-24" @default.
- W2056464524 creator A5001921296 @default.
- W2056464524 creator A5010446859 @default.
- W2056464524 creator A5013155553 @default.
- W2056464524 creator A5033210470 @default.
- W2056464524 creator A5045030058 @default.
- W2056464524 creator A5048877350 @default.
- W2056464524 creator A5070599968 @default.
- W2056464524 creator A5075997210 @default.
- W2056464524 creator A5076136934 @default.
- W2056464524 creator A5083383719 @default.
- W2056464524 date "2012-08-01" @default.
- W2056464524 modified "2023-10-04" @default.
- W2056464524 title "Fused bicyclic heteroarylpiperazine-substituted l-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group" @default.
- W2056464524 cites W1539796472 @default.
- W2056464524 cites W1553821695 @default.
- W2056464524 cites W1969974535 @default.
- W2056464524 cites W1981408121 @default.
- W2056464524 cites W1990399110 @default.
- W2056464524 cites W1998817071 @default.
- W2056464524 cites W2002352328 @default.
- W2056464524 cites W2011439711 @default.
- W2056464524 cites W2011778618 @default.
- W2056464524 cites W2012437459 @default.
- W2056464524 cites W2027157329 @default.
- W2056464524 cites W2027725447 @default.
- W2056464524 cites W2028707869 @default.
- W2056464524 cites W2034749948 @default.
- W2056464524 cites W2041933909 @default.
- W2056464524 cites W2047764904 @default.
- W2056464524 cites W2068563471 @default.
- W2056464524 cites W2081739151 @default.
- W2056464524 cites W2083473802 @default.
- W2056464524 cites W2106083318 @default.
- W2056464524 cites W2109157463 @default.
- W2056464524 cites W2120774442 @default.
- W2056464524 cites W2141264129 @default.
- W2056464524 cites W2155198744 @default.
- W2056464524 cites W2320246526 @default.
- W2056464524 cites W4230178491 @default.
- W2056464524 cites W4234825176 @default.
- W2056464524 doi "https://doi.org/10.1016/j.bmc.2012.06.033" @default.
- W2056464524 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22824762" @default.
- W2056464524 hasPublicationYear "2012" @default.
- W2056464524 type Work @default.
- W2056464524 sameAs 2056464524 @default.
- W2056464524 citedByCount "29" @default.
- W2056464524 countsByYear W20564645242012 @default.
- W2056464524 countsByYear W20564645242013 @default.
- W2056464524 countsByYear W20564645242014 @default.
- W2056464524 countsByYear W20564645242015 @default.
- W2056464524 countsByYear W20564645242016 @default.
- W2056464524 countsByYear W20564645242017 @default.
- W2056464524 countsByYear W20564645242018 @default.
- W2056464524 countsByYear W20564645242019 @default.
- W2056464524 countsByYear W20564645242020 @default.
- W2056464524 countsByYear W20564645242021 @default.
- W2056464524 countsByYear W20564645242022 @default.
- W2056464524 countsByYear W20564645242023 @default.
- W2056464524 crossrefType "journal-article" @default.
- W2056464524 hasAuthorship W2056464524A5001921296 @default.
- W2056464524 hasAuthorship W2056464524A5010446859 @default.
- W2056464524 hasAuthorship W2056464524A5013155553 @default.
- W2056464524 hasAuthorship W2056464524A5033210470 @default.
- W2056464524 hasAuthorship W2056464524A5045030058 @default.
- W2056464524 hasAuthorship W2056464524A5048877350 @default.
- W2056464524 hasAuthorship W2056464524A5070599968 @default.
- W2056464524 hasAuthorship W2056464524A5075997210 @default.
- W2056464524 hasAuthorship W2056464524A5076136934 @default.
- W2056464524 hasAuthorship W2056464524A5083383719 @default.
- W2056464524 hasConcept C118792377 @default.
- W2056464524 hasConcept C161790260 @default.
- W2056464524 hasConcept C178790620 @default.
- W2056464524 hasConcept C181199279 @default.
- W2056464524 hasConcept C185592680 @default.
- W2056464524 hasConcept C24961977 @default.
- W2056464524 hasConcept C2776980637 @default.
- W2056464524 hasConcept C2779240715 @default.
- W2056464524 hasConcept C50027330 @default.
- W2056464524 hasConcept C71240020 @default.
- W2056464524 hasConceptScore W2056464524C118792377 @default.
- W2056464524 hasConceptScore W2056464524C161790260 @default.
- W2056464524 hasConceptScore W2056464524C178790620 @default.
- W2056464524 hasConceptScore W2056464524C181199279 @default.
- W2056464524 hasConceptScore W2056464524C185592680 @default.
- W2056464524 hasConceptScore W2056464524C24961977 @default.
- W2056464524 hasConceptScore W2056464524C2776980637 @default.
- W2056464524 hasConceptScore W2056464524C2779240715 @default.
- W2056464524 hasConceptScore W2056464524C50027330 @default.
- W2056464524 hasConceptScore W2056464524C71240020 @default.
- W2056464524 hasIssue "16" @default.
- W2056464524 hasLocation W20564645241 @default.
- W2056464524 hasLocation W20564645242 @default.
- W2056464524 hasOpenAccess W2056464524 @default.
- W2056464524 hasPrimaryLocation W20564645241 @default.
- W2056464524 hasRelatedWork W1965959450 @default.
- W2056464524 hasRelatedWork W1982756588 @default.