Anti-Pneumocystis carinii pneumonia activity of dicationic carbazoles
摘要:
A series of 2,7- and 3,6-bis cationic carbazoles was synthesized and evaluated for activity against a rat model of Pneumocystis carinii pneumonia (PCP). The compounds were also tested for inhibition of topoisomerase II and binding to DNA. Several of the compounds proved to be more potent and less toxic than a standard anti-PCP drug (pentamidine). While no quantitative correlation was seen between anti-PCP activity, topoisomerase inhibition and DNA binding, a minimal level of DNA binding was found to be necessary for antimicrobial activity.
The present invention relates to a novel triscarbazole compound comprising cyclo- or polycycloalkyl or aralkyl substituent, which can be represented by Formula (I). wherein; RA is a substituent comprising a substituted or unsubstituted cyclo- or polycycloalkyl group wherein the ring system comprises three to twenty carbon atoms or an aralkyl group having an overall number of nine to twenty carbon atoms, RB, RC, RD and RE are any substituent other than a substituted or unsubstituted aniline, and m, o, p and q are same or different at each occurrence and represent an integer from 0 to 4.