Eudistomin derivatives, novel phosphodiesterase inhibitors: synthesis and relative activity

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Abstract
The preparations of novel phosphodiesterase inhibitors, 8-acetoxy-5-iodo-6-methoxypy rido[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 × 10−6, 3 × 10−6, 7 × 10−6 and 1 × 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.