4759-21-1Relevant academic research and scientific papers
A New Dioxazolone for the Synthesis of 1,2-Aminoalcohols via Iridium(III)-Catalyzed C(sp3)?H Amidation
Antien, Kevin,Baudoin, Olivier,Geraci, Andrea,Parmentier, Michael
supporting information, p. 22948 - 22955 (2021/09/09)
Vicinal aminoalcohols are widespread structural motifs in bioactive molecules. We report the development of a new dioxazolone reagent containing a p-nitrophenyldifluoromethyl group, which 1. displays a good safety profile; 2. shows a remarkably high react
Copper-Catalyzed Domino Reactions for the Synthesis of Phenothiazines
Huang, Manna,Huang, Dongting,Zhu, Xinhai,Wan, Yiqian
supporting information, p. 4835 - 4839 (2015/08/03)
A method for the one-pot synthesis of phenothiazines from benzothiazoles and aryl ortho-dihalides was explored. Preliminary work on the mechanism of the reaction suggested that it follows a domino process, including the hydrolysis of benzothiazoles followed by C-S coupling and C-N coupling. The low loading of the catalyst system (5 mol-% for both copper and ligand), the mild experimental conditions (90 °C, 12 h), and the use of a green reaction medium make this synthesis very attractive to academia and industry. A copper-catalyzed domino reaction consisting of the hydrolysis of benzothiazoles followed by C-S and C-N couplings for the synthesis of phenothiazines from benzothiazoles and aryl ortho-dihalides is described. The low loading of the catalyst system, mild experimental conditions, and the use of polyethylene glycol as the solvent make this synthetic approach very attractive to academia and industry.
Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure-activity relationship
Christensen, Mette K.,Erichsen, Kamille D.,Olesen, Uffe H.,Tj?rnelund, Jette,Fristrup, Peter,Thougaard, Annemette,Nielsen, S?ren Jensby,Sehested, Maxwell,Jensen, Peter B.,Loza, Einars,Kalvinsh, Ivars,Garten, Antje,Kiess, Wieland,Bj?rkling, Fredrik
supporting information, p. 9071 - 9088 (2014/01/06)
Existing pharmacological inhibitors for nicotinamide phosphoribosyltransferase (NAMPT) are promising therapeutics for treating cancer. By using medicinal and computational chemistry methods, the structure-activity relationship for novel classes of NAMPT inhibitors is described, and the compounds are optimized. Compounds are designed inspired by the NAMPT inhibitor APO866 and cyanoguanidine inhibitor scaffolds. In comparison with recently published derivatives, the new analogues exhibit an equally potent antiproliferative activity in vitro and comparable activity in vivo. The best performing compounds from these series showed subnanomolar antiproliferative activity toward a series of cancer cell lines (compound 15: IC50 0.025 and 0.33 nM, in A2780 (ovarian carcinoma) and MCF-7 (breast), respectively) and potent antitumor in vivo activity in well-tolerated doses in a xenograft model. In an A2780 xenograft mouse model with large tumors (500 mm3), compound 15 reduced the tumor volume to one-fifth of the starting volume at a dose of 3 mg/kg administered ip, bid, days 1-9. Thus, compounds found in this study compared favorably with compounds already in the clinic and warrant further investigation as promising lead molecules for the inhibition of NAMPT.
CONTROLLED RELEASE OF ACTIVE COMPOUNDS FROM DYNAMIC MIXTURES
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, (2010/09/17)
The present invention relates to a dynamic mixture in the form of a dynamic mixture obtained by reacting together, in the presence of water, at least one O-substituted hydroxylamine or S-substituted thiohydroxylamine derivative with at least one perfuming
Parasiticidal 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilides
Ali, Abdelselam,Altamore, Timothy M.,Bliese, Marianne,Fisara, Petr,Liepa, Andris J.,Meyer, Adam G.,Nguyen, Oahn,Sargent, Roger M.,Sawutz, David G.,Winkler, David A.,Winzenberg, Kevin N.,Ziebell, Angela
, p. 252 - 255 (2008/12/20)
A series of novel 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilide derivatives have shown significant in vitro parasiticidal activity against the ectoparasites Ctenocephalides felis and Rhipicephalus sanguineus. A number of these compounds also displayed significant in vitro endoparasite activity against the nematode Haemonchus contortus. Crown Copyright
Synthesis and opioid activities of some naltrexone oxime ethers
Mavunkel, B. J.,Rzeszotarski, W. J.,Kaplita, P. V.,DeHaven-Hudkins, D. L.
, p. 659 - 666 (2007/10/02)
A series of alkyl, cycloalkyl, aryl, and aralkyl ethers of naltrexone oxime was prepared.The compounds were examined in binding assays for μ, δ, and κ opioid receptor affinity.In addition, the naltrexone oxime ethers were studied in animal models that measure opioid agonist and antagonist activity.These studies led to the discovery of several compounds, notably phenethyl 3e and phenylpropyl 3f ethers of naltrexone, which have a 10-fold increase in potency at the κ opioid receptor with potent μ and κ agonist properties in vivo.naltrexone / oxime ether / opioid receptor / analgesia / receptor binding / kappa
