- Synthesis and catalytic activity of porous polymer containing ionic liquid structures
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A novel porous polymer containing ionic liquid (IL) structures was synthesized via quternization and condensation of 4-vinylpyridine and p-xylylene dichloride. The ionic liquid structures were incorporated in the polymeric framework and for this reason bulky IL molecules can hardly block pores and neutralize active sites. The polymer shows a high BET surface area and easily accessible active sites. Catalytically the polymer is very active in Michael additions with averaged yields over 96.0% achieved after short reaction times. The high BET surface, remarkable activity, operational simplicity, wide applicability and improved stability are the key properties of the polymer.
- Li, Junqiao,Lu, Wei,Li, Weifeng,Liang, Xuezheng
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p. 840 - 846
(2016/12/07)
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- Lipase-catalyzed aza-michael reaction on acrylate derivatives
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A methodology has been developed for an efficient and selective lipase-catalyzed aza-Michael reaction of various amines (primary and secondary) with a series of acrylates and alkylacrylates. Reaction parameters were tuned, and under the optimal conditions it was found that Pseudomonas stutzeri lipase and Chromobacterium viscosum lipase showed the highest selectivity for the aza-Michael addition to substituted alkyl acrylates. For the first time also, some CLEAs were examined that showed a comparable or higher selectivity and yield than the free enzymes and other formulations.
- Steunenberg, Peter,Sijm, Maarten,Zuilhof, Han,Sanders, Johan P. M.,Scott, Elinor L.,Franssen, Maurice C. R.
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p. 3802 - 3813
(2013/06/05)
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- N-Acylaminophenothiazines: Neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease
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We have previously reported the multifunctional profile of N-(3-chloro-10H-phenothiazin-10-yl)-3-(dimethylamino)propanamide (1) as an effective neuroprotectant and selective butyrylcholinesterase inhibitor. In this paper, we have developed a series of N-acylaminophenothiazines obtained from our compound library or newly synthesised. At micro- and sub-micromolar concentrations, these compounds selectively inhibited butyrylcholinesterase (BuChE), protected neurons against damage caused by both exogenous and mitochondrial free radicals, showed low toxicity, and could penetrate into the CNS. In addition, N-(3-chloro-10H-phenothiazin-10-yl)-2-(pyrrolidin-1-yl) acetamide (11) modulated the cytosolic calcium concentration and protected human neuroblastoma cells against several toxics, such as calcium overload induced by an l-type Ca2+-channel agonist, tau-hyperphosphorylation induced by okadaic acid and Aβ peptide.
- González-Mu?oz, Gema C.,Arce, Mariana P.,López, Beatriz,Pérez, Concepción,Romero, Alejandro,Barrio, Laura Del,Martín-De-Saavedra, María Dolores,Egea, Javier,León, Rafael,Villarroya, Mercedes,López, Manuela G.,García, Antonio G.,Conde, Santiago,Rodríguez-Franco, María Isabel
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p. 2224 - 2235
(2011/06/22)
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- Samarium(III) triflate catalyzed conjugate addition of amines to electron-deficient alkenes
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Amines undergo smooth nucleophilic addition to α,β-unsaturated compounds in the presence of a catalytic amount of samarium(III) triflate at ambient temperature to produce the corresponding β-amino compounds in excellent yields. This method is simple, convenient, and works efficiently under mild conditions. Georg Thieme Verlag Stuttgart.
- Yadav,Ramesh Reddy,Gopal Rao,Narsaiah,Subba Reddy
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p. 3447 - 3450
(2008/09/19)
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- Structure-activity relationship of trihexyphenidyl analogs with respect to the dopamine transporter in the on going search for a cocaine inhibitor
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A series of trihexyphenidyl (THP) analogs were used to search for a derivative that could serve as a cocaine inhibitor. A compound that blocks binding of the cocaine analog carboxyfluorotropane (CFT), allows dopamine uptake and exhibits low side effects could serve as a good candidate for that purpose. All analogs were tested for the extent to which they inhibit CFT binding, dopamine uptake and n-methyl scopolamine (NMS) binding. Several structure-function relationships emerged. Methylation/halogenation of THP's benzene ring enhanced the compound's ability to block CFT binding in comparison to its ability to block dopamine uptake (5a-e). Replacement of the cyclohexyl ring with a benzene ring tended to create compounds that had lower affinities to the dopamine transporter (7b compared to THP, 7d compared to 5h, 7c compared to 8c) and modification of THP's piperidine ring tended to enhance affinity to the dopamine transporter (5f-h, 8a, 8c). One analog (5f) that showed little muscarinic activity indicating that it would probably have few side effects was investigated for its effects as an in vivo cocaine inhibitor. However, it showed few antagonistic effects in vivo. Nevertheless, this work greatly elucidates the structure-function relationships required for potential cocaine inhibitors and so lays out promising directions for future research.
- Dar,Thiruvazhi,Abraham,Kitayama,Kopajtic,Gamliel,Slusher,Carroll,Uhl
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p. 1013 - 1021
(2007/10/03)
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