- Cyanoacetamide-based oxime carbonates: An efficient, simple alternative for the introduction of Fmoc with minimal dipeptide formation
-
Nowadays, most peptides are chemically achieved by using the Fmoc/tBu protection strategy, due to its fully orthogonal character, mild temporary group removal and resin cleavage steps. However, its introduction into N-unprotected amino acids is not exempt of synthetic inconveniences, such as dipeptide formation. Lately, novel oxime carbonates were introduced in the arsenal of reagents for the introduction of Fmoc, presenting almost negligible percentage of side-products. Herein, an enforced version of this family of Fmoc-carbonates is presented, containing stable and highly acidic cyanoacetamide-based oximes as leaving group. Such reactive species, affordable in only two steps from simple, readily available starting materials, show unusual ability to obtain the corresponding Fmoc-protected residues in high yield and minimal impact of detrimental side-products, mainly Fmoc-dipeptides.
- Khattab, Sherine N.,Subirós-Funosas, Ramon,El-Faham, Ayman,Albericio, Fernando
-
-
Read Online
- Design, synthesis and biological evaluation of certain CDK2 inhibitors based on pyrazole and pyrazolo[1,5-a] pyrimidine scaffold with apoptotic activity
-
Different series of novel pyrazole and pyrazolo[1,5-a] pyrimidine derivatives (2a-g), (3a-c), (7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit CDK2/cyclin A2 enzyme in vitro. In addition, the cytotoxicity of the newly synthesized compounds was screened against four different human cancer cell lines. The CDK2/cyclin A2 enzyme inhibitory activity revealed that compounds (2d) and (2 g) are among the most active with inhibitory activity values of 60% and 40%, respectively, while compounds (7d) and (10b) exhibited the highest activity among the newly synthesized derivatives against four tumor cell lines (HepG2, MCF-7, A549 and Caco2) with IC50 values 24.24, 14.12, 30.03 and 29.27 μM and 17.12, 10.05, 29.95 and 25.24 μM, respectively. Flow cytometry cell cycle assay was carried for compounds (7d) and (10b) to investigate their apoptotic activity. The obtained results revealed that they induced cell-cycle arrest in the G0-G1phase and reinforced apoptotic DNA fragmentation. Molecular modeling studies have been carried out to gain further understanding the binding mode of the target compounds together with field alignment to define the similar field properties.
- Ali, Ghada M.E.,Ibrahim, Diaa A.,Elmetwali, Amira M.,Ismail, Nasser S.M.
-
-
Read Online
- Synthesis and cytotoxic activity of chalcone analogues containing a thieno[2,3-d]pyrimidin-2-yl group as the A-ring or B-ring
-
Many natural or synthetic chalcones have potential anti-tumor activity. Here, we synthesized two series of chalcone analogues containing a thieno[2,3-d]pyrimidin-2-yl group and evaluated for their cytotoxic activity towards cultured human lung cancer A549 and colorectal HCT-116 cells. Among them, compound 8d was the most cytotoxic against HCT-116 cells, with an IC50 value of 2.65 μM. Analyses of the phenotypic changes induced by this compound found a dose-dependent accumulation of HCT-116 cells in sub-G1 phase, indicating that compound 8d might induce apoptosis. Furthermore, we found that 8d triggered mitochondrial membrane potential depolarization, promoted reactive oxygen species formation in HCT-116 cells, and increased the percentage of early and late apoptotic cells. Finally, immunoblotting indicated that 8d increased PARP-1 and caspases 3, 7 and 9 cleavage. These data suggest that compound 8d induces apoptosis via the mitochondrial death pathway.
- Wang, Fu-Cheng,Peng, Bin,Cao, Sheng-Li,Li, Hong-Yun,Yuan, Xiao-Li,Zhang, Ting-Ting,Shi, Ruifeng,Li, Zhuqing,Liao, Ji,Wang, Hailong,Li, Jing,Xu, Xingzhi
-
-
Read Online
- Rational design and synthesis of new PARP1 inhibitors
-
A preliminary simulation of bioactive compounds followed by their synthesis have been carried out: a set of new fragment PARP1 inhibitors - 3,5,6,7-tetrahydro-4H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-one derivatives - have been obtained. Molecular simulation has shown that binding is characterized by correlated hydrogen bonds with PARP1 and displacement of the highly-conservative water molecule by a polar group.
- Romashov, Leonid V.,Zeifman, Alexey A.,Zakharenko, Alexandra L.,Novikov, Fedor N.,Stroilov, Viktor S.,Stroganov, Oleg V.,Chilov, Germes G.,Khodyreva, Svetlana N.,Lavrik, Olga I.,Titov, Ilya Yu.,Svitan'Ko, Igor V.
-
-
Read Online
- Modulation of Nitrile Hydratase Regioselectivity towards Dinitriles by Tailoring the Substrate Binding Pocket Residues
-
The regioselective hydration of dinitriles is one of the most attractive approaches to prepare ω-cyanocarboxamides or diamides and such regioselectivity is often beyond the capability of chemical catalysts. The use of nitrile hydratase to biotransform dinitriles selectively would be highly desirable. Molecular docking of two aliphatic dinitriles and two aromatic dinitriles into the active site of a nitrile hydratase (NHase) from Rhodococcus rhodochrous J1 allowed the identification of proximal NHase substrate binding pocket residues. Four residues (βLeu48, βPhe51, βTyr68, and βTrp72) were selected for single- and double-point mutations to modulate the NHase regioselectivity towards dinitriles. Several NHase mutants with an altered regioselectivity were obtained, and the best one was Y68T/W72Y. Docking experiments further indicated that the poor binding affinity of aliphatic and aromatic ω-cyanocarboxamides to the NHase variants resulted in distinct regioselectivity between wild-type and mutated NHases.
- Cheng, Zhongyi,Cui, Wenjing,Xia, Yuanyuan,Peplowski, Lukasz,Kobayashi, Michihiko,Zhou, Zhemin
-
-
Read Online
- One-pot sequence for the decarboxylation of α-amino acids
-
Treatment of an α-amino acid with N-bromosuccinimide in water at pH 5 or in an alcoholic-aqueous ammonium chloride mixture, followed by addition of nickel(II) chloride and sodium borohydride, effected an overall decarboxylation via an intermediate nitrile to afford the corresponding amine in good yield.
- Laval, Gilles,Golding, Bernard T.
-
-
Read Online
- Synthesis and Docking Study of Novel Pyranocoumarin Derivatives
-
Abstract: A new series of fused tricyclic coumarin derivatives were designed, synthesized by a simple and convenient method, starting from 4-hydroxycoumarin and virtually screened by molecular docking on the target protein 3FRZ (PDB ID: 3FRZ), a HCV RNA-dependent RNA polymerase, for potency against hepatitis C virus (HCV). Efficient binding to the target protein was found for most of the synthesized compounds.
- Karteek, S. Durga,Reddy, A. Gopi,Tej, M. Bhuvan,Rao, M. V. Basaveswara
-
p. 272 - 282
(2021/04/02)
-
- Synthesis method of cyanoacetamide
-
The invention relates to a synthesis method of cyanoacetamide, and belongs to the technical field of organic synthesis. According to the method, a tubular reactor is used as reaction equipment, malonamide is used as a raw material, and cyanoacetamide is generated under the action of triphosgene. The triphosgene with relatively high reaction activity is used, so that the activation energy of the reaction can be reduced, and the forward proceeding of the reaction is promoted; a pipeline reactor is used as reaction equipment, so that the mass and heat transfer effect of a reaction system can be improved, the reaction time and the retention time of a product in the reaction system are further shortened, and the product purity and yield are effectively improved. The atom utilization rate is high, the by-product ammonium chloride can be sold as a product or used for other reactions, and the recovered solvent and the treated rectification base solution can be used for reactions; and only a small amount of activated carbon waste residues are generated, so that the environment-friendly benefit is high.
- -
-
Paragraph 0021-0030
(2021/08/25)
-
- Synthesis method of cyanoacetamide
-
The embodiment of the invention provides a cyanoacetamide synthesis method, which comprises the following steps: slowly adding liquid ammonia into a methyl cyanoacetate solution in a reaction environment of -10 DEG C to-5 DEG C; and after the reaction is completed, controlling the reaction environment to be within the range of -15 DEG C to-10 DEG C, and separating out cyanoacetamide crude crystals. Methyl cyanoacetate directly reacts with liquid ammonia, the liquid ammonia gasification step is reduced, and the reaction temperature is reduced. The reaction process is simple, and high reaction yield can be stably obtained.
- -
-
Paragraph 0024; 0060-0087
(2020/11/26)
-
- PROCESS FOR PREPARING CYANOACETATES
-
This invention relates to a process for producing cyanoacetates using asparagine as a precursor to cyanoacetamide, a staring material to form the cyanoacetates.
- -
-
Paragraph 0033; 0035
(2020/10/28)
-
- Structure-based design, synthesis and biological evaluation of a newer series of pyrazolo[1,5-a]pyrimidine analogues as potential anti-tubercular agents
-
In-depth study of structure-based drug designing can provide vital leads for the development of novel, clinically active molecules. In this present study, twenty six novel pyrazolo[1,5-a]pyrimidine analogues (6a-6z) were designed using molecular docking studies. The designed molecules were synthesized in good yields. Structural elucidation of the synthesized molecules was carried out using IR, MS, 1H NMR and 13C NMR spectroscopy. All the synthesized compounds were evaluated for their in-vitro anti-tubercular activity against H37Rv strain by Alamar Blue assay method. Most of the synthesized compounds displayed potent anti-tubercular activities. Amongst all the tested compounds 6p, 6g, 6n and 6h exhibited promising anti-tubercular activity. Further, these potent compounds were gauged for MDR-TB, XDR-TB and cytotoxic study. None of these compounds exhibited potent cytotoxicity. Stability of protein ligand complex was further evaluated by molecular dynamics simulation for 10 ns. All these results indicate that the synthesized compounds could be potential leads for further development of new potent anti-tubercular agents.
- Modi, Palmi,Patel, Shivani,Chhabria, Mahesh
-
p. 240 - 251
(2019/03/26)
-
- Chalcone analogue containing thieno[2,3-d]pyrimidine-2-yl, preparation method and uses thereof
-
The invention discloses a chalcone analogue containing thieno[2,3-d]pyrimidine-2-yl, wherein the chalcone analogue is represented by a general formula (I), and various substituents are defined in thespecification. The invention further discloses a preparation method of the compound. According to the present invention, the compound represented by the general formula (I) has inhibiting effects on the proliferation of human breast cancer cell lines (MFC-7 and MDA-MB-231), human cervical cancer cell lines (HeLa), human colon cancer cell lines (HCT-116 and HT-29) and human lung cancer cell lines (A549), has inhibiting effect on the proliferation of human hepatoma cell lines (HepG2), and can be used as an antitumor drug.
- -
-
Paragraph 0100-0102
(2020/01/03)
-
- Magnetic Nanoparticle-Supported Cu–NHC Complex as an Efficient and Recoverable Catalyst for Nitrile Hydration
-
Magnetic nanoparticles supported N-heterocyclic carbene–Cu complex was prepared and authenticated by FT-IR, SEM, EDX, VSM, powder-XRD. The catalytic activity of these magnetically retrievable NPs was investigated for hydration of nitriles as the simplest route for the synthesis of amides in an atom-economical manner. A wide range of nitriles containing various functional groups such as olefin, aldehyde, nitro, carboxylic acid was examined in this transformation to generate their corresponding amides in the aqueous medium. The immobilized catalyst was easily recovered using an external magnet and reused for six times without significant loss of its catalytic activity. Graphical Abstract: [Figure not available: see fulltext.].
- Kazemi Miraki, Maryam,Arefi, Marzban,Salamatmanesh, Arefeh,Yazdani, Elahe,Heydari, Akbar
-
p. 3378 - 3388
(2018/09/11)
-
- Synthesis of α-aminonitriles using aliphatic nitriles, α-amino acids, and hexacyanoferrate as universally applicable non-toxic cyanide sources
-
In cyanation reactions, the cyanide source is often directly added to the reaction mixture, which restricts the choice of conditions. The spatial separation of cyanide release and consumption offers higher flexibility instead. Such a setting was used for the cyanation of iminium ions with a variety of different easy-to-handle HCN sources such as hexacyanoferrate, acetonitrile or α-amino acids. The latter substrates were first converted to their corresponding nitriles through oxidative decarboxylation. While glycine directly furnishes HCN in the oxidation step, the aliphatic nitriles derived from α-substituted amino acids can be further converted into the corresponding cyanohydrins in an oxidative C-H functionalization. Mn(OAc)2 was found to catalyze the efficient release of HCN from these cyanohydrins or from acetone cyanohydrin under acidic conditions and, in combination with the two previous transformations, permits the use of protein biomass as a non-toxic source of HCN.
- Nauth, Alexander M.,Konrad, Tim,Papadopulu, Zaneta,Vierengel, Nina,Lipp, Benjamin,Opatz, Till
-
supporting information
p. 4217 - 4223
(2018/09/29)
-
- Development of novel tetrahydrothieno[2,3-c]pyridine-3-carboxamide based Mycobacterium tuberculosis pantothenate synthetase inhibitors: Molecular hybridization from known antimycobacterial leads
-
Twenty six 2,6-disubstituted 4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3- carboxamide derivatives were designed by molecular hybridization approach using and synthesized from piperidin-4-one by five step synthesis. Compounds were evaluated for Mycobacterium tuberculosis (MTB) pantothenate synthetase (PS) inhibition study, in vitro activities against MTB, cytotoxicity against RAW 264.7 cell line. Among the compounds, 6-(4-nitrophenylsulfonyl)-2-(5- nitrothiophene-2-carboxamido)-4,5,6,7-tetrahydrothieno[2,3-c] pyridine-3-carboxamide (11) was found to be the most active compound with IC50 of 5.87 ± 0.12 μM against MTB PS, inhibited MTB with MIC of 9.28 μM and it was non-cytotoxic at 50 μM. The binding affinity of the most potent inhibitor 11 was further confirmed biophysically through differential scanning fluorimetry.
- Samala, Ganesh,Devi, Parthiban Brindha,Nallangi, Radhika,Sridevi, Jonnalagadda Padma,Saxena, Shalini,Yogeeswari, Perumal,Sriram, Dharmarajan
-
p. 1938 - 1947
(2014/03/21)
-
- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
-
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
- -
-
Paragraph 0174 - 0175
(2014/05/24)
-
- Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach
-
Based on a known nanomolar Bcl-2 homology domain 3 (BH3) mimetic 3-thiomorpholin-8-oxo-8H-acenaphtho[1,2-b] pyrrole-9-carbonitrile (S1, MW: 331), we applied a fragment-based approach to obtain BH3 mimetics with improved affinity and improved solubility in a water-ethanol (9:1) cosolvent. After the deconstruction of 1 (S1), we obtained fragment cyanoacetamide (4), which was determined to be a ligand efficiency (LE) hot part. After a rational optimization through fragment evolution beginning with fragment 4, a smaller Mcl-1 inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g, MW: 288) with a 6-fold increase in affinity compared to 1 was obtained, as predicted by our optimization curve and identified by Mcl-1 protein nuclear magnetic resonance (NMR).
- Zhang, Zhichao,Song, Ting,Li, Xiangqian,Wu, Zhiyong,Feng, Yingang,Xie, Feibo,Liu, Chengwu,Qin, Jianquan,Chen, Hongbo
-
supporting information
p. 141 - 149
(2013/03/13)
-
- An efficient synthesis of 2-aminothiophenes via the gewald reaction catalyzed by an N-methylpiperazine-functionalized polyacrylonitrile fiber
-
A new N-methylpiperazine-functionalized polyacrylonitrile fiber has been developed to catalyze the Gewald reaction between 2,5-dihydroxy-1,4-dithiane and activated nitriles to afford 3-substituted 2-aminothiophenes in good to excellent yields (65-91%). Low catalyst loading (8.0 mol%), simple procedure, high yields, excellent recyclability, and reusability (up to 10 times with minimal loss of catalytic activity) are attractive features of this fiber catalyst. Georg Thieme Verlag Stuttgart · New York.
- Ma, Lichao,Yuan, Liwei,Xu, Changzhu,Li, Guowei,Tao, Minli,Zhang, Wenqin
-
supporting information
p. 45 - 52
(2013/03/13)
-
- 4-phenyl-α-cyanocinnamic acid amide: Screening for a negative ion matrix for MALDI-MS imaging of multiple lipid classes
-
Matrix-assisted laser desorption/ionization imaging mass spectrometry (MALDI-IMS) has become a method of choice in lipid analysis, as it provides localization information for defined lipids that is not readily accessible with nonmass spectrometric methods. Most current MALDI matrices have been found empirically. Nevertheless, preferential matrix properties for many analyte classes are poorly understood and may differ between lipid classes. We used rational matrix design and semiautomated screening for the discovery of new matrices suitable for MALDI-IMS of lipids. Utilizing Smartbeam- and nitrogen lasers for MALDI, we systematically compared doubly substituted α-cyanocinnamic acid derivatives (R1-CCA-R2) with respect to their ability to serve as negative ion matrix for various brain lipids. We identified 4-phenyl-α-cyanocinnamic acid amide (Ph-CCA-NH 2) as a novel negative ion matrix that enables analysis and imaging of various lipid classes by MALDI-MS. We demonstrate that Ph-CCA-NH2 displays superior sensitivity and reproducibility compared to matrices commonly employed for lipids. A relatively small number of background peaks and good matrix suppression effect could make Ph-CCA-NH2 a widely applicable tool for lipid analysis.
- Fueloep, Annabelle,Porada, Martina B.,Marsching, Christian,Blott, Henning,Meyer, Bjoern,Tambe, Suparna,Sandhoff, Roger,Junker, Hans-Dieter,Hopf, Carsten
-
p. 9156 - 9163
(2013/10/21)
-
- Synthesis of new 8-formyl-4-methyl-7-hydroxy coumarin derivatives
-
8-Formyl-4-Methyl-7-Hydroxy Coumarin Derivatives were synthesized via Penchem condensation followed by Duffs reaction. Treatment of this with N,N-di substituted cyano acetamides in the presence of piperdine afforded New 8- Formyl-4-Methyl-7-Hydroxy Coumarin Derivatives (7a-o). Their structures were characterized by IR, 1H and 13C NMR and Mass spectral and elemental analysis data.
- Manidhar,Rao, K. Uma Maheswara,Reddy, N. Bakthavatchala,Sundar, Ch. Syama,Reddy, C. Suresh
-
p. 459 - 463
(2012/11/07)
-
- BORON CONTAINING POLYBASIC BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTICS USES THEREOF
-
Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and theft methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent
- -
-
Page/Page column 56
(2012/08/28)
-
- Synthesis and antiviral bioactivities of 2-cyano-3-substitutedamino(phenyl) methylphosphonylacrylates (Acrylamides) containing alkoxyethyl moieties
-
An efficient reaction under microwave irradiation has been developed for the synthesis of a series of novel 2-cyano-3-substituted-amino(phenyl) methylphosphonylacrylates (acrylamides) II. The products obtained in shorter reaction time with moderate yields are fully characterized by elemental analysis, IR, 1H, 13C, and 31P NMR spectral data. The role of introducing various substituents and the effect of incorporating a-aminophosphonates with an alkoxyethyl moiety into the parent cyanoacrylate (acrylamide) structure are investigated. Among the studied compounds, both II-17 and II-24 displayed good in vivo curative, protection, and inactivation effects, which were comparable to those of the commercial reference ningnanmycin (inhibitory rates of 58.8, 60.2, 78.9% and 60.0, 58.9, 85.5%, respectively, at 500 mg/L against TMV). To the best of the authors' knowledge, this is the first report on the synthesis and antiviral activity of the title compounds II.
- Yang, Jia-Qiang,Song, Bao-An,Bhadury, Pinaki S.,Chen, Zhuo,Yang, Song,Xue-Jian, Cai,Hu, De-Yu,Xue, Wei
-
experimental part
p. 2730 - 2735
(2011/07/31)
-
- The synthesis and biological evaluation of some caffeic acid amide derivatives: E-2-Cyano-(3-substituted phenyl)acrylamides
-
A series of caffeic acid amide derivatives 2-cyano-(3-substituted phenyl)acrylamides were synthesized via Knoevenogal condensation of substituted benzaldehydes with cyanoacetamides. The structure of compound 1f was determined as E-isomer by X-ray diffractive analysis. The biological screening tests in vitro showed that compound 1b has obvious inhibitory activities against human gastric carcinoma cell line BGC-823, human nasopharyngeal carcinoma cell line KB and human hepatoma cell line BEL-7402 with IC50 values of 5.6 μg/mL, 13.1 μg/mL and 12.5 μg/mL, respectively. Some preliminary structure-activity relationships (SAR) were also proposed which may provide a direction for further study.
- Zhou, Wei,Li, Hai-bo,Xia, Chun-nian,Zheng, Xian-ming,Hu, Wei-xiao
-
scheme or table
p. 1861 - 1865
(2009/11/30)
-
- Synthesis and antiviral activities of cyanoacrylate derivatives containing an α-aminophosphonate moiety
-
Target compounds 8 were obtained by the reaction of alkyl 2-cyano-3,3-dimethylthioacrylate or cyarylamide (7a-7e) and α- aminobenzylphosphonate (5a-5e) under reflux condition using ethanol as solvent. Their structures were clearly verified by spectroscopic data (IR and 1H, 13C, and 31P NMR) and elemental analysis. These compounds were shown to be antivirally active in the bioassay. It was found that title compounds 8d and 8e had the same inactivation effect against tobacco mosaic virus (EC50 = 55.5 and 55.3 μg/mL) as the commercial product ningnanmycin (EC50 = 50.9 μg/mL). To the best of our knowledge, this is the first report on the synthesis and antiviral activity of cyanoacrylate derivatives containing an α-aminophosphonate moiety.
- Long, Ning,Cai, Xue-Jian,Song, Bao-An,Yang, Song,Chen, Zhuo,Bhadury, Pinaki S.,Hu, De-Yu,Jin, Lin-Hong,Xue, Wei
-
body text
p. 5242 - 5246
(2010/04/06)
-
- Synthesis of amides from esters and amines under microwave irradiation
-
Formamide, primary and secondary amines react with esters in the presence of potassium tert-butoxide under microwave irradiation. Substituted amides are formed in yields (generally more than 70%) much higher than under conventional heating.
- Zradni, Fatima-Zohra,Hamelin, Jack,Derdour, Aicha
-
p. 3525 - 3531
(2007/10/03)
-
- Process for preparing cyanoacetamide
-
Cyanoacetamide is prepared without additional catalyst by esterification of crude cyanoacetic acid with a monohydric alcohol which forms an azeotrope with water and has 4 to 10 carbon atoms, reacting the resulting ester with ammonia in the presence of a basic catalyst to give cyanoacetamide, and work-up by a mechanical separating operation and a thermal treatment.
- -
-
-
- Chemoenzymic Production of Lactams from Aliphatic α,ω-Dinitriles
-
Five- and six-membered ring lactams have been prepared by first converting an aliphatic α,ω-dinitrile to an ω-cyanocarboxylic acid ammonium salt, using a microbial cell catalyst having an aliphatic nitrilase activity (Acidovorax facilis 72W, ATCC 55746) or a combination of nitrile hydratase and amidase activities (Comamonas testosteroni 5-MGAM-4D, ATCC 55744). The ω-cyanocarboxylic acid ammonium salt was then directly converted to the corresponding lactam by hydrogenation in aqueous solution, without isolation of the intermediate ω-cyanocarboxylic acid or ω-aminocarboxylic acid. Only one of two possible lactam products was produced from α-alkyl-substituted α,ω-dinitriles, where the nitrilase of A. facilis 72W regioselectively hydrolyzed only the ω-cyano group to produce a single cyanocarboxylic acid ammonium salt in greater than 98% yield.
- Gavagan, John E.,Fager, Susan K.,Fallon, Robert D.,Folsom, Patrick W.,Herkes, Frank E.,Eisenberg, Amy,Hann, Eugenia C.,DiCosimo, Robert
-
p. 4792 - 4801
(2007/10/03)
-
- Inhibitors of the advanced glycosylation of proteins and methods of use therefor
-
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of an early glycosylation product of such target proteins resulting from their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
- -
-
-
- Inhibitors of the advanced glycosylation of proteins and methods of use therefor
-
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylatin. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
- -
-
-
- Kinetics and Mechanism of Copper(II)-catalysed Oxidation of Asparagine by Sodium N-Chloro-p-toluenesulphonamide in Alkaline Media
-
The kinetics of the CuII-catalysed chloraminometric oxidation of asparagine have been investigated in aqueous NaOH.The reaction rate is first order in chloramine-T and asparagine concentration and inverse first order in hydroxide ion concentration.The profile obtained from plots of observed rate constant against CuII ion concentration, indicates that the oxidation reaction proceeds through both uncatalysed and catalysed pathways.A negligible salt-effect and solvent-effect point to a mechanism involving a neutral molecule and anion in rate-determining step.The kinetic and thermodynamic parameters have been computed and suitable rate laws consistent with the experimental findings have been deduced.
- Sengar, Satish Kumar Singh,Yadav, B. S.
-
-
- Derivatives of 3-carboxy pyrid-2-ones
-
Novel compounds belonging to the class of 1-substituted benzylpyrid-2-one-4,6-dialkyl and 4,5,6-trisubstituted-3-carboxylic acids, amides, esters and physiologically acceptable salts. These compounds possess biological activity and in particular are gametocides and plant growth regulators. Novel 1-substituted benzyl-3-cyano-4,5,6-trisubstituted pyrid-2-ones are also disclosed as intermediates.
- -
-
-
