Kaizerman, Jacob A.; Gross, Matthew I.; Ge, Yigong; White, Sarah; Hu, Wenhao; Duan, Jian-Xin; Baird, Eldon E.; Johnson, Kirk W.; Tanaka, Richard D.; Moser, Heinz E.; Buerli, Roland W. published the artcile< DNA Binding Ligands Targeting Drug-Resistant Bacteria: Structure, Activity, and Pharmacology>, Electric Literature of 31166-29-7, the main research area is pyrrolecarboxamide trimeric aryl terminated preparation DNA binding antibacterial.
Potent DNA minor-groove binding antibacterials, e.g. I (R = aryl, heteroaryl), were designed based on the natural product distamycin A and synthesized, and their structure-activity relationship was investigated. These compounds have been shown to target A/T-rich sites within the bacterial genome and, as a result, inhibit DNA replication and RNA transcription. The optimization was focused on N-terminal aromatic heterocycles and C-terminal amines and resulted in compounds with improved in vivo tolerability and excellent in vitro antibacterial potency (MIC ≥ 0.031 μg/mL) against a broad range of Gram-pos. pathogens, including drug-resistant strains such as methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, and vancomycin-resistant Enterococcus faecalis. In a first proof-of-concept study, I (R = 3-chloro-2-thienyl) showed in vivo efficacy in a mouse peritonitis model against methicillin-sensitive S. aureus infection with an ED50 value of 30 mg/kg.
Journal of Medicinal Chemistry published new progress about Antimicrobial agents. 31166-29-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C5H2Cl2O2S, Electric Literature of 31166-29-7.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics