Eudistomin derivatives, novel phosphodiesterase inhibitors: Synthesis and relative activity

Article abstract of DOI:10.1111/j.2042-7158.1988.tb05154.x

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-hydroxypyridol[3,4-b]indole and 8-acetoxy-5-bromo-6-methoxypyrido[3,4-b]indole, are described together with concentrations giving 50% inhibition against cycle AMP phosphodiesterase, i.e. 3 x 10^-6, 3 x 10^-, 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.