Fabrizio Manetti

TL;DR: The screening of genomic libraries and whole-genome sequencing found that all the characterized mutants showed mutations in the mmpL3 gene, allowing us to conclude that resistance to BM212 maps to the MMPL3 protein, a member of the MmpL (mycobacterial membrane protein, large) family.

TL;DR: Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis and confirm the fundamental role of the p-chlorophenyl moiety at C4 in the antimycobacterial activity.

TL;DR: Two series of pyrazole derivatives were synthesized by parallel solution-phase synthesis and were assayed as inhibitors of Mycobacterium tuberculosis and showed high activity against MTB.

TL;DR: A series of new pyridazin-3(2H)-one derivatives were evaluated for their in vitro affinity toward both alpha(1)- and alpha(2)-adrenoceptors by radioligand receptor binding assays, and the polymethylene chain constituting the spacer between the furoylpiperazinyl pyridine and the arylpiperazine moiety was shown to influence the affinity and selectivity of these compounds.

TL;DR: The design and synthesis of new analogues of 1,5-chlorophenyl)-2-methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM212) are reported, showing that, although some nontuberculosis mycobacterial strains were found to be sensitive, MIC values were higher than those found toward MTB.