155375-23-8Relevant articles and documents
Catalytic, transition-metal-free semireduction of propiolamide derivatives: Scope and mechanistic investigation
Grams, R. Justin,Garcia, Christopher J.,Szwetkowski, Connor,Santos, Webster L.
, p. 7013 - 7018 (2020/09/12)
We report a transition-metal-free trans-selective semireduction of alkynes with pinacolborane and catalytic potassium tert-butoxide. A variety of 3-substituted primary and secondary propiolamides, including an analog of FK866, a potent nicotinamide mononucleotide adenyltransferase (NMNAT) inhibitor, are reduced to the corresponding (E)-3-substituted acrylamide derivatives in up to 99% yield with >99:1 E/Z selectivity. Mechanistic studies suggest that an activated Lewis acid-base complex transfers a hydride to the α-carbon followed by rapid protonation in a trans fashion.
Optimization and Evaluation of 5-Styryl-Oxathiazol-2-one Mycobacterium tuberculosis Proteasome Inhibitors as Potential Antitubercular Agents
Russo, Francesco,Gising, Johan,?kerbladh, Linda,Roos, Annette K.,Naworyta, Agata,Mowbray, Sherry L.,Sokolowski, Anders,Henderson, Ian,Alling, Torey,Bailey, Mai A.,Files, Megan,Parish, Tanya,Karlén, Anders,Larhed, Mats
, p. 342 - 362 (2015/06/30)
This is the first report of 5-styryl-oxathiazol-2-ones as inhibitors of the Mycobacterium tuberculosis (Mtb) proteasome. As part of the study, the structure-activity relationship of oxathiazolones as Mtb proteasome inhibitors has been investigated. Furthermore, the prepared compounds displayed a good selectivity profile for Mtb compared to the human proteasome. The 5-styryl-oxathiazol-2-one inhibitors identified showed little activity against replicating Mtb, but were rapidly bactericidal against nonreplicating bacteria. (E)-5-(4-Chlorostyryl)-1,3,4-oxathiazol-2-one) was most effective, reducing the colony-forming units (CFU)/mL below the detection limit in only seven days at all concentrations tested. The results suggest that this new class of Mtb proteasome inhibitors has the potential to be further developed into novel antitubercular agents for synergistic combination therapies with existing drugs.
Pharmaceutical applications of hydrotropic agents, polymers thereof, and hydrogels thereof
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, (2008/06/13)
The present invention is directed to compounds effective for increasing the water solubility of poorly soluble drugs. Hydrotropic agents are identified, such as for increasing the solubility of paclitaxel. Polymerizable monomers of the hydrotropic agents