Matches in SemOpenAlex for { <https://semopenalex.org/work/W79551429> ?p ?o ?g. }
Showing items 1 to 81 of
81
with 100 items per page.
- W79551429 abstract "There are two structural differences between the positive inotropes amrinone (A) and milrinone (M): (1) M has a pyridone 2-methyl substituent and; (2) the pyridone 5-amino substituent of A is replaced with a nitrile in M. SAR studies confirmed that the 2-methyl substituent is responsible for the dramatically increased potency of M relative to A (canine i.v. ED/sub 50/'s=37 and 1891 ..mu..g/kg, respectively). Both M and A inhibited canine heart PDEase III (IC/sub 50/'s=12 and 150..mu..M, respectively). Moreover, in a series of M/A congeners, the correlation between in vitro PDEase III IC/sub 50/'s and in vivo inotropic ED/sub 50/'s was highly significant (r = 0.98, p < 0.01). In the crystal-state, the methyl substituent of M induces a marked alteration in its 3-dimensional topology relative to A. They have now completely assigned the /sup 13/C- and /sup 1/H-NMR spectra of A and M and have used the chemical shifts of the pyridone C-4 protons as conformational reporters. These studies revealed that the C-4 protons of methyl containing congeners (M-like) experience a 0.38-0.53 ppm upfield shift relative to the corresponding proton resonance in unmethylated congeners (A-like). These data suggest there are marked, methyl-induced differences in the solution conformations of A and more » M. « less" @default.
- W79551429 created "2016-06-24" @default.
- W79551429 creator A5003400580 @default.
- W79551429 creator A5004152370 @default.
- W79551429 creator A5006900371 @default.
- W79551429 creator A5052712439 @default.
- W79551429 creator A5070545695 @default.
- W79551429 date "1986-03-05" @default.
- W79551429 modified "2023-09-28" @default.
- W79551429 title "Studies on solution conformations and mechanism of action of amrinone and milrinone" @default.
- W79551429 hasPublicationYear "1986" @default.
- W79551429 type Work @default.
- W79551429 sameAs 79551429 @default.
- W79551429 citedByCount "0" @default.
- W79551429 crossrefType "journal-article" @default.
- W79551429 hasAuthorship W79551429A5003400580 @default.
- W79551429 hasAuthorship W79551429A5004152370 @default.
- W79551429 hasAuthorship W79551429A5006900371 @default.
- W79551429 hasAuthorship W79551429A5052712439 @default.
- W79551429 hasAuthorship W79551429A5070545695 @default.
- W79551429 hasConcept C115624301 @default.
- W79551429 hasConcept C121332964 @default.
- W79551429 hasConcept C1276947 @default.
- W79551429 hasConcept C134018914 @default.
- W79551429 hasConcept C155647269 @default.
- W79551429 hasConcept C155710745 @default.
- W79551429 hasConcept C178790620 @default.
- W79551429 hasConcept C185592680 @default.
- W79551429 hasConcept C2776645727 @default.
- W79551429 hasConcept C2778689049 @default.
- W79551429 hasConcept C2779240715 @default.
- W79551429 hasConcept C2779739782 @default.
- W79551429 hasConcept C4839761 @default.
- W79551429 hasConcept C67787023 @default.
- W79551429 hasConcept C71240020 @default.
- W79551429 hasConcept C71924100 @default.
- W79551429 hasConcept C8010536 @default.
- W79551429 hasConceptScore W79551429C115624301 @default.
- W79551429 hasConceptScore W79551429C121332964 @default.
- W79551429 hasConceptScore W79551429C1276947 @default.
- W79551429 hasConceptScore W79551429C134018914 @default.
- W79551429 hasConceptScore W79551429C155647269 @default.
- W79551429 hasConceptScore W79551429C155710745 @default.
- W79551429 hasConceptScore W79551429C178790620 @default.
- W79551429 hasConceptScore W79551429C185592680 @default.
- W79551429 hasConceptScore W79551429C2776645727 @default.
- W79551429 hasConceptScore W79551429C2778689049 @default.
- W79551429 hasConceptScore W79551429C2779240715 @default.
- W79551429 hasConceptScore W79551429C2779739782 @default.
- W79551429 hasConceptScore W79551429C4839761 @default.
- W79551429 hasConceptScore W79551429C67787023 @default.
- W79551429 hasConceptScore W79551429C71240020 @default.
- W79551429 hasConceptScore W79551429C71924100 @default.
- W79551429 hasConceptScore W79551429C8010536 @default.
- W79551429 hasLocation W795514291 @default.
- W79551429 hasOpenAccess W79551429 @default.
- W79551429 hasPrimaryLocation W795514291 @default.
- W79551429 hasRelatedWork W158930958 @default.
- W79551429 hasRelatedWork W1968196227 @default.
- W79551429 hasRelatedWork W1969608219 @default.
- W79551429 hasRelatedWork W1969789862 @default.
- W79551429 hasRelatedWork W1976785957 @default.
- W79551429 hasRelatedWork W1980566146 @default.
- W79551429 hasRelatedWork W1983670779 @default.
- W79551429 hasRelatedWork W1990477206 @default.
- W79551429 hasRelatedWork W2009572038 @default.
- W79551429 hasRelatedWork W2015287830 @default.
- W79551429 hasRelatedWork W2019508420 @default.
- W79551429 hasRelatedWork W2040765521 @default.
- W79551429 hasRelatedWork W2043177456 @default.
- W79551429 hasRelatedWork W2058934473 @default.
- W79551429 hasRelatedWork W2104102016 @default.
- W79551429 hasRelatedWork W2171602608 @default.
- W79551429 hasRelatedWork W2260736268 @default.
- W79551429 hasRelatedWork W2283974770 @default.
- W79551429 hasRelatedWork W2336742517 @default.
- W79551429 hasRelatedWork W2339761604 @default.
- W79551429 isParatext "false" @default.
- W79551429 isRetracted "false" @default.
- W79551429 magId "79551429" @default.
- W79551429 workType "article" @default.