265107-43-5Relevant articles and documents
Design of adenosine kinase inhibitors from the NMR-based screening of fragments
Hajduk,Gomtsyan,Didomenico,Cowart,Bayburt,Solomon,Severin,Smith,Walter,Holzman,Stewart,McGaraughty,Jarvis,Kowaluk,Fesik
, p. 4781 - 4786 (2000)
A strategy is described for designing high-affinity ligands using information derived from the NMR-based screening of fragments. The method involves the fragmentation of an existing lead molecule, identification of suitable replacements for the fragments, and incorporation of the newly identified fragments into the original scaffold. Using this technique, novel substituents were rapidly identified and incorporated into lead inhibitors of adenosine kinase that exhibited potent in vitro and in vivo activities. This approach is a valuable strategy for modifying existing leads to improve their potency, bioavailability, or toxicity profile and thus represents a useful technique for lead optimization.
Compound capable of effectively inhibiting or killing multi-drug resistant bacteria and preparation method and application of compound
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Paragraph 0182; 0691, (2017/06/02)
The invention discloses a compound capable of effectively inhibiting or killing bacterial microorganisms. The compound has a structural general formula shown as the formula I (please see the formula in the description). Pharmacodynamic experiments prove that the compound can effectively inhibit or kill the broad-spectrum and multi-drug resistant staphylococcus aureus, streptococcus pneumoniae and staphylococcus aureus and is expected to be developed into a novel effective antibacterial drug with new targets.
INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 71-72, (2010/02/14)
The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.