Eudistomin derivatives, novel phosphodiesterase inhibitors: synthesis and relative activity.
The preparations of novel phosphodiesterase inhibitors, 8-acetoxy-5-iodo-6-methoxypyrido[3,4-b]indole, 5,7-dibromo-6-hydroxypyrido[3,4-b]indole, 5,7-dichloro-6-hydroxypyrido[3,4-b]-indole and 8-acetoxy-5-bromo-6-methoxypyrido[3,4-b]indole, are described together with concentrations giving 50% inhibition against cyclic AMP phosphodiesterase, i.e. 3 X 10(-6), 3 X 10(-6), 7 X 10(-6) and 1 X 10(-5) M, respectively. The relative potency of these eudistomin derivatives is discussed in terms of the chemical structures compared with those of other inactive eudistomins and derivatives.
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors; D000818:Animals; D002417:Cattle; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D009206:Myocardium / Q000201:enzymology; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D014561:Urochordata / Q000378:metabolism
D007211:Indoles; D010726:Phosphodiesterase Inhibitors; D015105:3',5'-Cyclic-AMP Phosphodiesterases