ANTIMICROBIAL ACTIVITIES OF INDOLOCARBAZOLE AND BIS-INDOLE PROTEIN-KINASE-C INHIBITORS .2. SUBSTITUTION ON MALEIMIDE NITROGEN WITH FUNCTIONAL-GROUPS BEARING A LABILE HYDROGEN

New compounds, structurally related to the potent protein kinase C inh ibitor staurosporine, and substituted on the imide nitrogen with a fun ctional group bearing a labile hydrogen (hydroxymethyl, amino, hydroxy ), were synthesized. Their in vitro inhibitory potencies towards prote in kinase C and protein kinase A showed that N-hydroxymethyl and N-hyd roxy substitution, unlike alkyl substitution, can provide efficient pr otein kinase C inhibitors. The antimicrobial activities of these new c ompounds against Streptomyces chartreusis and Streptomyces griseus, Ba cillus cereus, Escherichia coli, Candida albicans and Botrytis cinerea were examined. They proved to be inactive against E. coli and two fun gi. The results suggest that there is no link between in vitro inhibit ion of protein kinase C and inhibition of growth and sporulation of th e two Streptomyces tested. Unlike indolocarbazole maleimides, bis-indo le maleimides are active against the two Streptomyces species.