15850-20-1Relevant academic research and scientific papers
Solvent-Free Synthesis, ADME Prediction, and Evaluation of Antibacterial Activity of Novel Sulfonamide Derivatives
Rafiee Pour,Nazifi,Afshari Safavi,Nazifi,Massah
, p. 852 - 859 (2019)
A series of novel sulfonamides containing a 2-amino-1,3-thiazole fragment have been synthesized using a simple and efficient method under solvent-free conditions. The obtained N-(4-sulfamoyl-1,3-thiazol-2-yl)-4-nitrobenzamides were evaluated for their ant
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)- 3,5-difluorobenzoylimino]-thiazol-3-ylmethyl} Ester (Lu AA47070): A phosphonooxymethylene prodrug of a potent and selective hA2A receptor antagonist
Sams, Anette G.,Mikkelsen, Gitte K.,Larsen, Mogens,Langg?rd, Morten,Howell?, Mark E.,Schr?der, Tenna J.,Brennum, Lise T.,Torup, Lars,J?rgensen, Erling B.,Bundgaard, Christoffer,Kreilg?rd, Mads,Bang-Andersen, Benny
supporting information; experimental part, p. 751 - 764 (2011/04/18)
The discovery and structure-activity relationship of a series of hA 2A receptor antagonists is described. Compound 28 was selected from the series as a potent and selective compound and was shown to be efficacious in an in vivo model of Parkinson's disease. It had acceptableADME properties; however, the low intrinsic solubility of this compound was limiting for its developability, because the oral bioavailability from dosing in suspension was significantly lower than the oral bioavailability from solution dosage. As a consequence, prodrugs of 28 were prepared with dramatically increased aqueous solubility. The prodrugs efficiently delivered 28 into systemic circulation, with no detectable levels of prodrug in plasma samples. From this investigation, we selected 32 (Lu AA47070), a phosphonooxymethylene prodrug of 28, as a drug candidate.
Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors
Altmeyer, Markus A.,Marschner, Aline,Schiffmann, Rolf,Klein, Christian D.
supporting information; experimental part, p. 4038 - 4044 (2010/08/20)
Inhibitors of methionine aminopeptidases (MetAPs) are treatment options for various pathological conditions. Several inhibitor classes have been described previously, but only few data on the subtype selectivity, which is of crucial importance for these enzymes, is available. We present a systematic study on the subtype- and species-selectivity of MetAP inhibitors that require the binding of an auxiliary metal ion. This includes, in particular, compounds based on the benzimidazole pharmacophore, but also hydroxyquinoline and picolinic acid derivatives. Our data indicates that a significant degree of selectivity can be attained with metal-dependent MetAP inhibitors.
PRO-DRUGS OF N-THIAZOL-2YL-BENZAMIDE DERIVATIVES
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Page/Page column 34, (2010/11/24)
The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
N-THIAZOL-2-YL-BENZAMIDE DERIVATIVES
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Page/Page column 17-18, (2008/06/13)
The invention relates to N-thiazol-2-yl-benzamide derivatives of the formula I in the description wherein the variables are as defined in the claims. The compounds are A2A-receptor ligands, such as antagonists, agonists, reverse agonists or partial agonists, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
Ring-opened analogs of indomethacin affecting human neutrophil functions
Andreani, Aldo,Leoni, Alberto,Locatelli, Alessandra,Morigi, Rita,Rambaldi, Mirella,Gehret, Jean-Claude,Traniello, Serena,Cariani, Alessio,Spisani, Susanna
, p. 299 - 312 (2007/10/03)
A series of ring-opened analogs of indomethacin was synthesized and tested in vitro (at concentrations ranging from 10-9 to 10-5 mol/1) on human neutrophil functions. Two compounds lacking the carboxylic group were subjected to the s
