Synthesis and inotropic activity of hydroindene derivatives.
A synthetic approach to hydroindenic inotropic agents has been developed, starting from enantiopure Hajos-Parrish (1). Hajos-Wiechert (2), and related diketones. Their transformation into C-1 formyl derivatives and other subsequent synthetic targets is described. The results of the thermodynamic equilibration between both epimers of each formyl derivative are analysed. The inotropic activities of selected compounds on right and left atrial preparations are also evaluated and discussed.
Sevillano
L G
LG
Laboratorio de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, Spain.
Melero
C P
CP
Boya
M
M
López
J L
JL
Tomé
F
F
Caballero
E
E
Carrón
R
R
Montero
M J
MJ
Medarde
M
M
Feliciano
A S
AS
D000818:Animals; D016275:Atrial Function; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D066298:In Vitro Techniques; D007192:Indenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D013329:Structure-Activity Relationship
D002316:Cardiotonic Agents; D007192:Indenes