Matches in SemOpenAlex for { <https://semopenalex.org/work/W2949424897> ?p ?o ?g. }
Showing items 1 to 77 of
77
with 100 items per page.
- W2949424897 abstract "The effectiveness of phosphonamidate peptide analogues as inhibitors of rat kidney or human brain metalloendopeptidase (enkephalinase, E.C. 3.4.24.11) and angiotensin-converting enzyme (ACE, 3.4.14.1) has been explored with a series of enkephalin analogues in which the scissile Gly3-Phe4 amide bond has been replaced with a phosphonamidate moiety. These compounds exhibited good inhibitory potency against enkephalinase with several of the analogues having Ki values in the submicromolar range as contrasted to micromolar or higher toward ACE. Within a series of [(N-acylamino)methyl] phosphonamidates there was a dramatic decrease in inhibitory activity against enkephalinase as the N-acyl moiety was substituted with larger, more hydrophobic acyl groups. Likewise, the inhibitory activity of the [(N-acylamino)methyl] phosphonamidates against ACE was attenuated by larger phenylalkyl acyl functionalities, although not to the same degree as against enkephalinase. However, phosphonamidate pentapeptide analogues of (Leu)enkephalin and (D-Ala2,D-Leu5)enkephalin showed good inhibitory potency against both enzymes. Interestingly, these two (Leu)enkephalin phosphonamidate analogues were completely inactive in the electrically stimulated guinea pig ileum and mouse vas deferens preparations. Conformational factors that may be involved in this inactivity are discussed." @default.
- W2949424897 created "2019-06-27" @default.
- W2949424897 creator A5012767879 @default.
- W2949424897 creator A5054083436 @default.
- W2949424897 creator A5070230820 @default.
- W2949424897 creator A5074369828 @default.
- W2949424897 date "1985-12-24" @default.
- W2949424897 modified "2023-09-24" @default.
- W2949424897 title "ChemInform Abstract: SYNTHESIS AND BIOLOGICAL EVALUATION OF PHOSPHONAMIDATE PEPTIDE INHIBITORS OF ENKEPHALINASE AND ANGIOTENSIN-CONVERTING ENZYME" @default.
- W2949424897 cites W1985287732 @default.
- W2949424897 doi "https://doi.org/10.1002/chin.198551305" @default.
- W2949424897 hasPublicationYear "1985" @default.
- W2949424897 type Work @default.
- W2949424897 sameAs 2949424897 @default.
- W2949424897 citedByCount "0" @default.
- W2949424897 crossrefType "journal-article" @default.
- W2949424897 hasAuthorship W2949424897A5012767879 @default.
- W2949424897 hasAuthorship W2949424897A5054083436 @default.
- W2949424897 hasAuthorship W2949424897A5070230820 @default.
- W2949424897 hasAuthorship W2949424897A5074369828 @default.
- W2949424897 hasConcept C170493617 @default.
- W2949424897 hasConcept C181199279 @default.
- W2949424897 hasConcept C185592680 @default.
- W2949424897 hasConcept C2776568683 @default.
- W2949424897 hasConcept C2776980637 @default.
- W2949424897 hasConcept C2777803847 @default.
- W2949424897 hasConcept C2779138802 @default.
- W2949424897 hasConcept C2779281246 @default.
- W2949424897 hasConcept C2780919550 @default.
- W2949424897 hasConcept C2781063702 @default.
- W2949424897 hasConcept C2781372283 @default.
- W2949424897 hasConcept C31684184 @default.
- W2949424897 hasConcept C45197812 @default.
- W2949424897 hasConcept C55493867 @default.
- W2949424897 hasConcept C71240020 @default.
- W2949424897 hasConceptScore W2949424897C170493617 @default.
- W2949424897 hasConceptScore W2949424897C181199279 @default.
- W2949424897 hasConceptScore W2949424897C185592680 @default.
- W2949424897 hasConceptScore W2949424897C2776568683 @default.
- W2949424897 hasConceptScore W2949424897C2776980637 @default.
- W2949424897 hasConceptScore W2949424897C2777803847 @default.
- W2949424897 hasConceptScore W2949424897C2779138802 @default.
- W2949424897 hasConceptScore W2949424897C2779281246 @default.
- W2949424897 hasConceptScore W2949424897C2780919550 @default.
- W2949424897 hasConceptScore W2949424897C2781063702 @default.
- W2949424897 hasConceptScore W2949424897C2781372283 @default.
- W2949424897 hasConceptScore W2949424897C31684184 @default.
- W2949424897 hasConceptScore W2949424897C45197812 @default.
- W2949424897 hasConceptScore W2949424897C55493867 @default.
- W2949424897 hasConceptScore W2949424897C71240020 @default.
- W2949424897 hasLocation W29494248971 @default.
- W2949424897 hasOpenAccess W2949424897 @default.
- W2949424897 hasPrimaryLocation W29494248971 @default.
- W2949424897 hasRelatedWork W1956534786 @default.
- W2949424897 hasRelatedWork W1964258286 @default.
- W2949424897 hasRelatedWork W1964518833 @default.
- W2949424897 hasRelatedWork W1985287732 @default.
- W2949424897 hasRelatedWork W1992883810 @default.
- W2949424897 hasRelatedWork W1999299369 @default.
- W2949424897 hasRelatedWork W1999788794 @default.
- W2949424897 hasRelatedWork W2017544249 @default.
- W2949424897 hasRelatedWork W2037827717 @default.
- W2949424897 hasRelatedWork W2042019970 @default.
- W2949424897 hasRelatedWork W2047605799 @default.
- W2949424897 hasRelatedWork W2067127117 @default.
- W2949424897 hasRelatedWork W2073632860 @default.
- W2949424897 hasRelatedWork W2080688470 @default.
- W2949424897 hasRelatedWork W2085331866 @default.
- W2949424897 hasRelatedWork W2087803629 @default.
- W2949424897 hasRelatedWork W2091834659 @default.
- W2949424897 hasRelatedWork W2094801912 @default.
- W2949424897 hasRelatedWork W2411018403 @default.
- W2949424897 hasRelatedWork W2951560224 @default.
- W2949424897 isParatext "false" @default.
- W2949424897 isRetracted "false" @default.
- W2949424897 magId "2949424897" @default.
- W2949424897 workType "article" @default.