Hydroxyacyl derivatives of forskolin--their positive inotropic activity.
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).].
Lal
B
B
Department of Chemistry, Hoechst Marion Roussel Limited, Mumbai, India. bansilal@hoechstres.rpgms.ems.vsnl.net.in
Gangopadhyay
A K
AK
Rajagopalan
R
R
Ghate
A V
AV
D000215:Acylation; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D005576:Colforsin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects* / Q000502:physiology; D006325:Heart Atria; D006900:Hydroxylation; D066298:In Vitro Techniques; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D009200:Myocardial Contraction / Q000187:drug effects*; D013329:Structure-Activity Relationship
D005576:Colforsin