37136-97-3Relevant academic research and scientific papers
Quaternary Ammonium Trifluoromethoxide Salts as Stable Sources of Nucleophilic OCF3
Britton, Robert,Friesen, Chadron M.,Jelier, Benson J.,Martin, Rainer E.,Meanwell, Michael,Newton, Josiah J.
supporting information, p. 1785 - 1790 (2020/03/24)
The reaction of nucleophilic tertiary amines with trifluoromethyl and pentafluoroethyl methyl ethers provides quaternary ammonium trifluoromethoxide (NR4OCF3) and pentafluoroethoxide (NR4OCF2CF3) salts, respectively, in good yields. The new trifluoromethoxide salts disclosed herein are uniquely stable for extended periods of time in both the solid state and in solution, which complements contemporary reagents. Here we describe the preparation of a range of NR4OCF3 salts, their long-term stability, and utility in substitution reactions.
Aryloxazolidinediones: Identification of potent orally active PPAR dual α/γ agonists
Desai, Ranjit C.,Gratale, Dominick F.,Han, Wei,Koyama, Hiroo,Metzger, Edward,Lombardo, Victoria K.,MacNaul, Karen L.,Doebber, Thomas W.,Berger, Joel P.,Leung, Kwan,Franklin, Ronald,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 3541 - 3544 (2007/10/03)
A series of novel aryloxazolidine-2,4-diones was synthesized. A structure-activity relationship study of these compounds led to the identification of potent, orally active PPAR dual α/γ agonists. Based on the results of efficacy studies in the db/db mice
Compounds enhancing antitumor activity of other cytotoxic agents
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, (2008/06/13)
This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).
A novel nonpeptide HIV-1 protease inhibitor: Elucidation of the binding mode and its application in the design of related analogs
Lunney,Hagen,Domagala,Humblet,Kosinski,Tait,Warmus,Wilson,Ferguson,Hupe,Tummino,Baldwin,Bhat,Liu,Erickson
, p. 2664 - 2677 (2007/10/02)
HIV-1 protease has been identified as a significant target enzyme in AIDS research. While numerous peptide-derived inhibitors have been described, the identification of a nonpeptide inhibitor remains an important goal. Using an HIV-1 protease mass screening technique, 4-hydroxy-3-(3-phenoxypropyl)-2H-1- benzopyran-2-one (1) was identified as a nonpeptide competitive inhibitor of the enzyme. Employing a Monte Carlo-based docking procedure, the coumarin was docked in the active site of the enzyme, revealing a binding mode that was later confirmed by the X-ray crystal analysis. Several analogs were prepared to test the binding interactions and improve the overall binding affinity. The most active compound in the study was 4,7-dihydroxy-3-[4-(2- methoxyphenyl)butyl]-2H-1-benzopyran-2-one (31).
