104189-85-7Relevant articles and documents
Benzimidazoles as NMDA glycine-site antagonists: Study on the structural requirements in 2-position of the ligand
Dannhardt, Gerd,Kohl, Beate K.
, p. 123 - 129 (2000)
A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 μM (9 b) and 38.0 μM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazol-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen revealed new insights into the importance of amide functionalities within the heterocycle for the affinity of antagonist glycine-site ligands.
SYNTHESIS OF N-CARBOXYALKYLBENZIMIDAZOLIN-2-ONES
Khalikov, S. S.,Kadyrov, Ch. Sh.,Ayupova, A. T.,Molchanov, L. V.
, p. 1251 - 1254 (1985)
The corresponding N-mono and N,N'-dicarboxyalkylbenzimidazolin-2-ones were prepared by the reaction of the sodium salts of benzimidazolin-2-one and its 1,5,6-substituted derivatives with chloroacetic acid, acrylonitrile. and γ-butyrolactone.
THIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
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Page/Page column 116, (2008/06/13)
The invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, which are antagonist of the CXCR3 chemokine receptor useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
Ramoplanin derivatives possessing antibacterial activity
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Page/Page column 67, (2010/11/23)
Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.