- Is CuII Coordinated to Patellamides inside Prochloron Cells?
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Dinuclear CuII–patellamide complexes (patellamides are naturally occurring cyclic pseudo-octapeptides) are known to be efficient catalysts for hydrolysis reactions of biological importance, for example, those of phosphatase, carbonic anhydrase, and glycosidase. However, the biological role of patellamides is still unknown. Patellamides were originally extracted from the sea squirt Lissoclinum patella, but are now known to be ribosomally expressed by the blue-green algae Prochloron that live in symbiosis with L. patella. In a further step to unravel the metabolic significance of the patellamide complexes, the question as to whether these are also formed inside Prochloron cells is addressed. In this study, a biocompatible patellamide–fluorescent dye conjugate has been introduced into living Prochloron cells and, by means of flow cytometry and confocal microscopy, it is shown that CuII ions are coordinated to patellamides in vivo.
- Comba, Peter,Eisenschmidt, Annika,Gahan, Lawrence R.,Herten, Dirk-Peter,Nette, Geoffrey,Schenk, Gerhard,Seefeld, Martin
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Read Online
- Transmembrane H+/Cl- cotransport activity of bis(amido)imidazole receptors
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A series of sickle-shaped bis(amido) imidazoles are synthesized for their ion transport studies. Proton-anion binding by the neutral and protonated form of receptors assessed by 1H-NMR titration experiments confirmed better chloride binding by the protonated form of a receptor compared to its neutral form. The transport experiments across unimolecular vesicles (by HPTS and lucigenin assays) confirmed the H+/Cl- symport process under the applied pH gradient conditions. The transporter also allows anion antiport as evident from the studies under symmetrical pH conditions. The ionophoric activity by the mobile carrier mechanism is proved by the U-tube experiment.
- Shinde, Sopan Valiba,Talukdar, Pinaki
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p. 4483 - 4490
(2019/05/16)
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- Stable isotope labeled 3-methyl-quinoxaline-2-carboxylic acid and synthesis method thereof
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The invention discloses a stable isotope labeled 3-methyl-quinoxaline-2-carboxylic acid and a synthesis method thereof. The synthesis method comprises the following steps: S1, acetoacetate reacts withnitrite under the catalysis of organic acid to obtain 2-hydroxyimino-acetoacetate; s2, condensing the 2-hydroxyimino-acetoacetate with stable isotope labeled aniline under the catalysis of acetic acid, and then adding phosphorus oxychloride to react to obtain isotope labeled 3-methyl-quinoxaline-2-carboxylate; s3, hydrolyzing the stable isotope labeled 3-methyl-quinoxaline-2-carboxylic acid esterunder alkaline conditions, adjusting the pH value to acidity after the reaction is finished, and precipitating the stable isotope labeled 3-methyl-quinoxaline-2-carboxylic acid from the aqueous solution. The synthesis method not only has low preparation cost and few experimental steps, but also has purity and isotope abundance of more than 98%, and can be completely used as an internal standard for detecting 3-methyl-quinoxaline-2-carboxylic acid, thus greatly reducing detection cost.
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Paragraph 0032; 0033
(2019/10/01)
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- Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators
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Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinyl imidazoles series of mGlu5 receptor negative allosteric modulators (mGluR5 NAMs) using a functional cell-based assay is described in this Letter. Analysis of the Ligand-lipophilic efficiency (LipE) of compounds provided new insight for the design of potent mGluR5 negative allosteric modulators with anti-depressant activities.
- Chae, Eunhee,Shin, Yong-Je,Ryu, Eun-Ju,Ji, Mi Kyung,Ryune Cho, Nahm,Lee, Ki-Ho,Jeong, Hyun Ji,Kim, Soo-Jin,Choi, Yeonjung,Seok Oh, Kyung,Park, Chun-Eung,Soo Yoon, Young
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p. 2134 - 2139
(2013/05/09)
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- Stereoselective Lewis base-catalyzed asymmetric hydrosilylation of α-acetamido-β-enamino esters: Straightforward approach for the construction of α,β-diamino acid derivatives
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The Lewis base-organocatalyzed asymmetric hydrosilylation of α-acetamido-β-enamino esters was investigated. Among various chiral Lewis base catalysts, a novel catalyst derived from L-serine was found to be the most efficient one which can promote the reaction to afford a series of α,β-diamino acid derivatives with high yields (up to 99%), excellent enantioselectivities (up to 98% ee) and moderate diastereoselectivities (up to 80:20 dr). The absolute configuration of one of the products was determined by the X-ray crystallographic analysis. In addition, the mechanism and the transition state of the reaction were proposed. Copyright
- Jiang, Yan,Chen, Xing,Hu, Xiao-Yan,Shu, Chang,Zhang, Yong-Hong,Zheng, Yong-Sheng,Lian, Chun-Xia,Yuan, Wei-Cheng,Zhang, Xiao-Mei
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supporting information
p. 1931 - 1936
(2013/08/23)
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- Nitrite ionic liquids (IL-ONO and [bmim]NO2) as effective nitrosonium sources for the synthesis of α-oximinoketones under mild heterogeneous conditions
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Ketones and β-diketones were nitrosated and converted to their corresponding α-oximinoketones using task-specific ionic liquids, 1-(4-nitritobutyl)-3-methylimidazolium chloride, IL-ONO, and 1-butyl-3-methylimidazolium nitrite at room temperature. The results from two ionic liquids are comparable and showed that these IL's are effective nitrosonium sources for the preparation of oximinoketones. The protocol is rapid, the yields are excellent, and the method is simple. Copyright
- Valizadeh,Shomali,Gholipour
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experimental part
p. 163 - 166
(2012/03/10)
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- Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies
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The synthesis and structure-activity relationship studies of imidazoles are described. The target compounds 6-20 represent a novel chemotype of potent and CB2/CB1 selective cannabinoid CB2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P and calculated polar surface area values. Compound 12 exhibited the highest CB2 receptor affinity (Ki = 1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold).
- Lange, Jos H.M.,van der Neut, Martina A.W.,Wals, Henri C.,Kuil, Gijs D.,Borst, Alice J.M.,Mulder, Arie,den Hartog, Arnold P.,Zilaout, Hicham,Goutier, Wouter,van Stuivenberg, Herman H.,van Vliet, Bernard J.
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supporting information; experimental part
p. 1084 - 1089
(2010/06/11)
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- Solution versus fluorous versus solid-phase synthesis of 2,5-disubstituted 1,3-azoles. Preliminary antibacterial activity studies
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(Chemical Equation Presented) A small library of compounds with an oxa(thia)zole scaffold and structural diversity in both positions 2 and 5 has been synthesized. Double acylation of a protected glycine affords intermediate α-amido-β-ketoesters, which in turn can be dehydrated to afford 1,3-oxazoles or reacted with Lawesson's reagent to furnish 1,3-thiazoles. This procedure was designed with its adaptation to fluorous techniques in mind. Thus, when a protected glycine with a fluorous tag in the ester moiety is used as a starting material, the synthesis can be easily completed without column chromatography purification of intermediate compounds with good to excellent yields, thus affording a suitable entry to the preparation of small libraries of these bioactive compounds. The prepared oxa(thia)zoles were assayed for their antibacterial activity, and several of them were active against Staphylococcus aureus.
- Sanz-Cervera, Juan F.,Blasco, Rauel,Piera, Julio,Cynamon, Michael,Ibanez, Ignacio,Murguia, Marcelo,Fustero, Santos
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supporting information; experimental part
p. 8988 - 8996
(2010/03/24)
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- 1H-imidazole derivatives as cannabinoid CB2 receptor modulators
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The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
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Page/Page column 19
(2008/06/13)
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- BICYCLIC PYRAZOLE DERIVATIVE
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A compound represented by the following formula (I), a prodrug thereof, or a pharmaceutically acceptable salt of either. These are compounds having high DPP-IV inhibitory activity and improved in safety, nontoxicity, etc. (I) [In the formula, R1 represents hydrogen, optionally substituted alkyl, etc.; the solid line and dotted line between A1 and A2 indicate a double bond (A1=A2), etc.; A1 represents a group represented by the formula C(R2), etc.; A2 represents a group represented by the formula C(R4), etc.; R2 represents hydrogen, optionally substituted alkyl, etc.; R4 represents hydrogen, optionally substituted alkyl, etc.; R6 represents hydrogen, optionally substituted aryl, etc.; and -Y represents, e.g.; a group represented by the formula (A): (A) (wherein ml is 0, 1, 2, or 3; and R7 is absent, or one or two R7's are present and each independently represents optionally substituted alkyl, etc.).]
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Page/Page column 172-173
(2010/11/30)
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- NOVEL COMPOUNDS AS AGONIST FOR PPAR GAMMA AND PPAR ALPHA, METHOD FOR PREPARATION OF THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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The present invention relates to novel compounds accelerating the activity of Peroxisome proliferator-activated receptor gamma (PPARγ) and alpha (PPARα), processes of preparing the same, and pharmaceutical compositions containing the same as an active agent.
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Page/Page column 114
(2010/02/11)
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- Zinc-induced deoximation of α,α′-dioxo-type oximes and oxime ethers leading to α,β-diketo esters
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The deoximation of a variety of α,α′-dioxo-type oximes and oxime ethers was achieved under mild conditions using zinc/AcOH, which gave good yields of α,β-diketo esters.
- Ryu, Ilhyong,Kuriyama, Hiroki,Miyazato, Hironari,Minakata, Satoshi,Komatsu, Mitsuo,Yoon, Joo-Yong,Kim, Sunggak
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p. 1407 - 1408
(2007/10/03)
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- ASYMMETRIC SYNTHESIS. PRACTICAL PRODUCTION OF D AND L THREONINE. DYNAMIC KINETIC RESOLUTION IN RHODIUM AND RUTHENIUM CATALYZED HYDROGENATION OF 2-ACYLAMINO-3-OXOBUTYRATES.
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Enantioselective syntheses of D and L threonine are described.Racemic methyl and ethyl 2-acylamino-3-oxobutyrate 1 were synthesized from the corresponding acetoacetates 6 and then hydrogenated stereoselectively via dynamic kinetic resolution with various chiral P * P Rh(I) 8 and Ru(II) 10 catalysts to give syn optically active alcohols which could be converted by hydrolysis and treatment with propylene oxide into threonine.The best results were obtained using (-) CHIRAPHOS Ru and (+) BINAP Ru as catalysts, in the hydrogenation step leading respectively to D threonine (ee : 99percent) and L threonine (ee : 94percent) in 26-34percent overall yields.
- Genet, J.P.,Pinel, C.,Mallart, S.,Juge, S.,Thorimbert, S.,Laffitte, J.A.
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p. 555 - 567
(2007/10/02)
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