108402-07-9Relevant academic research and scientific papers
PHARMACOLOGICALLY ACTIVE COMPOUNDS
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Paragraph 00136, (2015/07/15)
The present invention relates to compounds of formula (I) shown below: wherein Q is as defined herein. The compounds of formula (I) act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.
A cleavable linker based on the levulinoyl ester for activity-based protein profiling
Geurink, Paul P.,Florea, Bogdan I.,Li, Nan,Witte, Martin D.,Verasdonck, Joeri,Kuo, Chi-Lin,Van Der Marel, Gijs A.,Overkleeft, Herman S.
supporting information; experimental part, p. 6802 - 6805 (2010/12/25)
(Chemical Equation Presented) Get linked: The title linker is stable under various biological conditions and can be cleaved chemoselectively with hydrazine (see scheme). Its use is demonstrated in the activity-based enrichment and identification of proteasome active subunits from cell extracts.
2,4-Diamino-5-benzylpyrimidines and Analogues as Antibacterial Agents. 9. Lipophilic Trimethoprim Analogues as Antigonococcal Agents
Roth, B.,Baccanari, D. P.,Sigel, C. W.,Hubbell, J. P.,Eaddy, J.,et al.
, p. 122 - 129 (2007/10/02)
Lipophilic analogues of trimethoprim (1) bearing 3,5-dialkyl-4-hydroxy substituents in the benzene ring are much more active in vitro against Neisseria gonorrhoeae than is 1.The 3,5-diisopropyl-4-hydroxy derivative (2) was selected as a candidate for clinical evaluation as an antigonococcal agent, and as part of the preliminary evaluation it was submitted to extended pharmacokinetic and metabolism studies in dogs.Although the compound was not extensively conjugated by metabolic enzymes, one of the methyl groups was metabolized to produce a 3-isopropyl-4-hydroxy-5-(α-carboxyethyl)benzyl derivative (43), which was rapidly excreted.Related analogues were likewise extensively metabolized.
