Hydroxyacyl derivatives of forskolin--their positive inotropic activity

B Lal; A K Gangopadhyay; R Rajagopalan; A V Ghate

doi:10.1016/s0968-0896(98)00123-0

Hydroxyacyl derivatives of forskolin--their positive inotropic activity

Bioorg Med Chem. 1998 Nov;6(11):2061-73. doi: 10.1016/s0968-0896(98)00123-0.

Authors

B Lal¹, A K Gangopadhyay, R Rajagopalan, A V Ghate

Affiliation

¹ Department of Chemistry, Hoechst Marion Roussel Limited, Mumbai, India. [email protected]

PMID: 9881097
DOI: 10.1016/s0968-0896(98)00123-0

Abstract

Using appropriate protection and deprotection sequence novel hydroxyacyl chains of the type CO(CH2)nOH are synthesized and are utilized to develop new analogues of forskolin. Several compounds showed good positive inotropic activity. Compound 12 is almost 10 times more active than forskolin (EC50 = 0.002 microgram/ml).].

MeSH terms

Acylation
Animals
Blood Pressure / drug effects
Colforsin / analogs & derivatives*
Colforsin / chemical synthesis*
Colforsin / chemistry
Colforsin / pharmacology
Guinea Pigs
Heart / drug effects*
Heart / physiology
Heart Atria
Hydroxylation
In Vitro Techniques
Models, Molecular
Molecular Conformation
Molecular Structure
Myocardial Contraction / drug effects*
Structure-Activity Relationship

Substances

Colforsin