42514-50-1Relevant academic research and scientific papers
Reaction of 4,4-dimethyl-1,3-dioxane with dinitriles
Kuznetsov,Mazepa,Brusilovskii,Krasnoshchekaya
, p. 126 - 127 (2001)
The reaction of 4,4-dimethyl-1,3-dioxane with bis(2-cyano)diethyl ether or 1,2-di(β-cyanoethoxy)-ethane yields the corresponding bis[2-(4,4-dimethyl-5,6-dihydro-2-oxazinyl)]diethyl ether and 1,2-di{β-[2-(4,4-dimethyl-5,6-dihydro-2-oxazinyl)]ethoxy} ethane
Structure stability/activity relationships of sulfone stabilized N,N-dichloroamines
Low, Eddy,Kim, Bum,Francavilla, Charles,Shiau, Timothy P.,Turtle, Eric D.,O'Mahony, Donogh J.R.,Alvarez, Nichole,Houchin, Ashley,Xu, Ping,Zuck, Meghan,Celeri, Chris,Anderson, Mark B.,Najafi, Ramin,Jain, Rakesh K.
scheme or table, p. 3682 - 3685 (2011/08/06)
Structure stability/activity relationships (SXR) of a new class of N,N-dichloroamine compounds were explored to improve antimicrobial activity against Escherichia coli, Staphylococcus aureus, and Candida albicans while maintaining aqueous solution stability. This study identified a new class of solution-stable and topical antimicrobial agents. These agents are sulfone-stabilized and possess either a quaternary ammonium or sulfonate appendages as a water solubilizing group. Several unique challenges were confronted in the synthesis of these novel compounds which are highlighted in the discussion.
N,N-Dichloroaminosulfonic acids as novel topical antimicrobial agents
Low, Eddy,Nair, Satheesh,Shiau, Timothy,Belisle, Barbara,Debabov, Dmitri,Celeri, Chris,Zuck, Meghan,Najafi, Ron,Georgopapadakou, Nafsika,Jain, Rakesh
scheme or table, p. 196 - 198 (2009/05/07)
2-Dichloroamino-2-methyl-propane-1-sulfonic acid sodium salt (2a), a stable derivative of endogenous N,N-dichlorotaurine (1), has been identified and is under development as a topical antimicrobial agent. Structure-activity relationships of analogs were explored to achieve optimal antimicrobial activity with minimal mammalian toxicity while maintaining the desired stability. All the analogs synthesized showed antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Candida albicans in the range of 1-128 μg/mL and cytotoxicity against mammalian L929 cells in the range 80-1900 μg/mL.
Novel acetylcholine and carbamoylcholine analogues: Development of a functionally selective α4β2 nicotinic acetylcholine receptor agonist
Hansen, Camilla P.,Jensen, Anders A.,Christensen, Jeppe K.,Balle, Thomas,Liljefors, Tommy,Fr?lund, Bente
experimental part, p. 7380 - 7395 (2009/12/07)
A series of carbamoylcholine and acetylcholine analogues were synthesized and characterized pharmacologically at neuronal nicotinic acetylcholine receptors (nAChRs). Several of the compounds displayed low nanomolar binding affinities to the α4β2 nAChR and pronounced selectivity for this subtype over α3β4, α4β4, and α7 nAChRs. The high nAChR activity of carbamoylcholine analogue 5d was found to reside in its R-enantiomer, a characteristic most likely true for all other compounds in the series. Interestingly, the pronounced α4β2 selectivities exhibited by some of the compounds in the binding assays translated into functional selectivity. Compound 5a was a fairly potent partial α4β2 nAChR agonist with negligible activities at the α3β4 and α7 subtypes, thus being one of the few truly functionally selective α4β 2 nAChR agonists published to date. Ligand-protein docking experiments using homology models of the amino-terminal domains of α4β2 and α3β4 nAChRs identified residues Val111(β2)/Ile113(β4) , Phe119(β2)/Gln121(β4), and Thr155(α4)/Ser150(α3) as possible key determinants of the α4β2/α 3β4-selectivity displayed by the analogues.
Aminoquinolones as GSK-3 inhibitors
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Page/Page column 102, (2008/06/13)
Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.
Bicyclicpyrimidones and their use to treat diseases
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, (2008/06/13)
The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest.
Pyrrolotriazinone compounds and their use to teat diseases
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, (2008/06/13)
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
PYRROLOTRIAZINONE COMPOUNDS AND THEIR USE TO TREAT DISEASES
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Page 94, (2010/02/04)
The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
Reaction of 1,3-dioxanes with acetone cyanohydrin
Kuznetsov,Brusilovskii
, p. 574 - 575 (2007/10/03)
The reaction of 4-phenyl- and 4,4-dimethyl-1,3-dioxanes with acetone cyanohydrin leads to hydrolytically unstable 2-(1-hydroxy-1-methylethyl)-5,6-dihydro-1,3-oxazines, which are readily saponified in alkaline medium to the corresponding 1,3-amino alcohols
Synthesis of N-protected 14C-labelled (2E)-5-amino-5-methylhex-2-enoic acid analogues
Jessen, Claus U.,Selvig, Helle,Valsborg, Jacob S.
, p. 265 - 275 (2007/10/03)
A novel method of preparing N-protected (2E)-5-amino-5-methylhex-2-enoic acids has been developed based on the synthesis of 3-methyl-3-amino-butanol. The method was used to synthesise 14C-labelled compounds of (1) via synthesis of triethylphosphono[1-14C]acetate.
