Ye, Jiqing published the artcileDiscovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors, Quality Control of 1885-29-6, the main research area is antibacterial RNA polymerase sigma factor interaction inhibition.
Formation of a bacterial RNA polymerase (RNAP) holoenzyme by a catalytic core RNAP and a sigma (σ) initiation factor is essential for bacterial viability. As the primary binding site for the housekeeping σ factors, the RNAP clamp helix domain represents an attractive target for novel antimicrobial agent discovery. Previously, we designed a pharmacophore model based on the essential amino acids of the clamp helix, such as R278, R281, and I291 (Escherichia coli numbering), and identified hit compounds with antimicrobial activity that interfered with the core-σ interactions. In this work, we rationally designed and synthesized a class of triaryl derivatives of one hit compound and succeeded in drastically improving the antimicrobial activity against Streptococcus pneumoniae, with the min. inhibitory concentration reduced from 256 to 1μg/mL. Addnl. characterization of antimicrobial activity, inhibition of transcription, in vitro pharmacol. properties, and cytotoxicity of the optimized compounds demonstrated their potential for further development.
Journal of Medicinal Chemistry published new progress about Acinetobacter baumannii. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Quality Control of 1885-29-6.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts