605658-32-0Relevant articles and documents
MODULATORS OF TLR3/DSRNA COMPLEX AND USES THEREOF
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Page/Page column 33-34, (2012/08/07)
The present invention provides compounds and compositions that can modulate formation of Toll-like receptor 3 (TLR3) and double-stranded RNA (dsRNA) complex, and methods for using the same. In particular, some aspects of the invention provide compounds of the formula (I) compositions comprising and methods for using the same, where n, Ar1, Ar2, X1, X2, X3, Z1, and Z2 are those defined herein.
DNA binding ligands targeting drug-resistant bacteria: Structure, activity, and pharmacology
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.,Bürli, Roland W.
, p. 3914 - 3929 (2007/10/03)
We describe the lead optimization and structure-activity relationship of DNA minor-groove binding ligands, a novel class of antibacterial molecules. 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-positive pathogens, including drug-resistant strains such as methicillin-resistant Stapylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and vancomycin-resistant Enterococcus faecalis (VRE). In a first proof-of-concept study, a selected compound (35) showed in vivo efficacy in a mouse peritonitis model against methicillin-sensitive S. aureus infection with an ED50 value of 30 mg/kg.
