Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.

Drug-resistant infections are an emergent threats to safety to many populations, specially in the III World countries. WHO is particularly concerned about bacterial resistance among Gram negative pathogens. Previous rigid benzo[a]dihydrocarbazole showed poor antibacterial activity against Gram positive and Gram negative bacteria. The aims of this research was to sinthesise new benzo[b]carbazole structures based on tetracycline pharmacophore scaffold to enhance antimicrobial activity and to reduce toxicity associated to tetracyclines.
In patent License AR20110103126 two potential benzo[b]carbazole lead candidates have been designed by in silico modeling techniques(or skills????). The antibacterial activity was assessed against Gram positive and Gram negative bacteria. Both compounds showed antibacterial activity against Gram positive and moderate activity against Gram negative and Candida albicans at µM level (1-8 µM). In silico and in vivo toxicological activity were performed and no alerts were observed. These results suggest us that flexible compounds may open new perspectives for future antimicrobial research.