- A selective separation of amino acid functionalized ion liquid, preparation method and its application
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The invention discloses a functionalized ionic liquid for modifying lipase, the structure of the functionalized ionic liquid is shown as formula (I), wherein M is 1 ~ 2; R1 and R2 are independently selected from substituted or unsubstituted alkyl, and the
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Paragraph 0060; 0061; 0062
(2016/10/10)
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- Discovery of new heterocycles with activity against human neutrophile elastase based on a boron promoted one-pot assembly reaction
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Herein we demonstrate for the first time that a boron promoted one-pot assembly reaction may be used to discover novel enzyme inhibitors. Inhibitors for HNE were simply assembled in excellent yields, high diastereoselectivities and IC50 up to 1
- Montalbano, Francesco,Cal, Pedro M. S. D.,Carvalho, Marta A. B. R.,Gon?alves, Lídia M.,Lucas, Susana D.,Guedes, Rita C.,Veiros, Luís F.,Moreira, Rui,Gois, Pedro M. P.
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supporting information
p. 4465 - 4472
(2013/08/23)
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- Studies of β-turn opening with model peptides containing non-coded α-amino isobutyric acid
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Single crystal X-ray diffraction studies show that among the three terminally protected model tripeptides I-III, Boc-Ile-Aib-Xx-OMe (Xx in peptide I: Val; II: Leu; III: Phe) with a centrally placed non-coded amino acid Aib (Aib: α-amino isobutyric acid), peptide I displays a conformational preference for β-turn, peptide II forms a hydrated β-turn representing the solvent mediated intermediate for the interconversion between β-turn and β-strand and peptide III adopts a completely unfolded β-strand like structure. By varying the steric bulk of the third residue, Xx(3), various conformations related to the structural interconversion between the β-turn and β-strand have been isolated. The peptide conformations in the solution phase have been probed by solvent dependent NMR titration and CD spectroscopy. Morphological studies with scanning electron microscopy (SEM) reveal that among the three peptides only peptide III can form filamentous fibrils in the solid state.
- Dutt, Anita,Dutta, Arpita,Mondal, Raju,Spencer, Elinor C.,Howard, Judith A.K.,Pramanik, Animesh
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p. 10282 - 10289
(2008/02/13)
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- Quantitative structure-activity relationships of pine weevil antifeedants, a multivariate approach
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Antifeedant activity of mainly phenylpropanoic, cinnamic, and benzoic acids esters was tested on the pine weevil, Hylobius abietis (L.). Of 105 compounds screened for activity, 9 phenylpropanoates, 3 cinnamates, and 4 benzoates were found to be highly active antifeedants. To understand the structure-activity relationships of these compounds, a multivariate analysis study was performed. A number of molecular and substituent descriptors were calculated and correlated to results from two-choice feeding tests with H. abietis. Three local models were developed that had good internal predictive ability. External test sets showed moderate predictivity. In general, low polarity, small size, and high lipophilicity were characteristics for compounds having good antifeedant activity.
- Sunnerheim, Kerstin,Nordqvist, Anneli,Nordlander, Goeran,Borg-Karlson, Anna-Karin,Unelius, C. Rickard,Bohman, Bjoern,Nordenhem, Henrik,Hellqvist, Claes,Karlen, Anders
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p. 9365 - 9372
(2008/03/17)
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- The use of bifunctional catalyst systems in the asymmetric addition of alkynylzinc to aldehydes
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The bifunctional ligand 2a showed a more enhanced reactivity than that of the corresponding amino alcohol ligand in the asymmetric addition of alkynylzinc to benzaldehyde. The bifunctional ligand 2a can catalyze the addition of phenylacetylene to various
- Kang, Yong-Feng,Liu, Lei,Wang, Rui,Yan, Wen-Jin,Zhou, Yi-Feng
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p. 3155 - 3159
(2007/10/03)
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- An efficient strategy for the synthesis of chiral liquid crystals using Evans' methodology
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The synthesis of liquid crystal compound 2 was achieved using Evans' methodology. The strategy was based on three key synthetic reactions: alkylation of chiral amide enolates, Mitsunobu and, finally, esterification. The final compound presents a stable smectic A phase.
- Merlo, Aloir A.,Fernandes, Mirele S.
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p. 1167 - 1178
(2007/10/03)
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- Organocatalytic asymmetric conjugate addition of nitroalkanes to α,β-unsaturated enones using novel imidazoline catalysts
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A new catalytic enantioselective conjugate addition of nitroalkanes to acyclic α,β-unsaturated enones catalyzed by novel organic catalysts has been developed. A series of chiral amines has been tested as catalysts for the addition of 2-nitropropane to benzylideneacetone, and it is found that a novel imidazoline catalyst, prepared from phenylalanine, can catalyze a highly enantioselective 1,4addition reaction. The reaction of various acyclic and cyclic nitroalkanes was found to proceed well with enantioselectivities up to 86% ee, and enantiopure products can be obtained by recrystallization. The potential of the reaction is documented by the reaction of a series of substituted α,β-unsaturated enones with different nitroalkanes. Furthermore, the synthetic applicability of the reaction is demonstrated by the formation of optically active functionalized pyrrolines and pyrrolidines by reductive amination of the products. On the basis of the absolute configuration of the conjugate addition products, the mechanism for the reaction is discussed and a transition state proposed.
- Halland, Nis,Hazell, Rita G.,Jorgensen, Karl Anker
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p. 8331 - 8338
(2007/10/03)
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