In search of novel water soluble forskolin analogues for positive inotropic activity

In search of novel water soluble forskolin analogues for positive inotropic activity

Using the novel lead from hydroxy acetyl substituted forskolin analogues, such as 7β-hydroxyacetyl-7β-deacetyl forskolin or 6β-hydroxyacetyl forskolin, a number of water soluble ω-amino acyl derivatives were synthesized. Two such compounds 6 and 18 showed better in vitro activity but failed to show...

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Veröffentlicht in:Bioorganic & medicinal chemistry 1998-11, Vol.6 (11), p.2075-2083
Hauptverfasser: Lal, Bansi, Gangopadhyay, Ashok Kumar, Gidwani, Ramesh M., Fernandes, Magno, Rajagopalan, Ramanujam, Ghate, Anil Vasantrao
Format: Artikel
Sprache:eng
Schlagworte:
2-hydroxy acetyl
Acetylation
Animals
Blood Pressure - drug effects
Cats
Colforsin - analogs & derivatives
Colforsin - chemical synthesis
Colforsin - chemistry
Colforsin - pharmacology
Forskolin
Guinea Pigs
Heart - drug effects
Heart - physiology
Heart Atria
Hydroxylation
In Vitro Techniques
Indicators and Reagents
Myocardial Contraction - drug effects
Myocardial Contraction - physiology
positive inotropic activity
Solubility
Structure-Activity Relationship
Water
ω-aminoacyl
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Zusammenfassung:Using the novel lead from hydroxy acetyl substituted forskolin analogues, such as 7β-hydroxyacetyl-7β-deacetyl forskolin or 6β-hydroxyacetyl forskolin, a number of water soluble ω-amino acyl derivatives were synthesized. Two such compounds 6 and 18 showed better in vitro activity but failed to show in vivo activity.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(98)00124-2