Ricerc@Sapienza

This minireview surveys the work of our research group directed toward finding novel antimycobacterial and anti-inflammatory drugs. Many active compounds were found with a common 1,5-diarylpyrrole skeleton. Some of the synthesized compounds, designed on the basis of structure–activity relationship studies, showed very interesting activities and proved to be effective in vivo, thus providing evidence of their attractiveness for lead optimization.

BM635 is the hit compound of a promising anti-TB compound class. Herein we report systematic variations
around the central pyrrole core of BM635 and we describe the design, synthesis, biological
evaluation, pharmacokinetic analysis, as well as in vivo TB mouse efficacy studies of novel BM635 analogues
that show improved physicochemical properties. This hit-to-lead campaign led to the identification
of a new analogue, 4-((1-isopropyl-5-(4-isopropylphenyl)-2-methyl-1H-pyrrol-3-yl)methyl)