Org. and Biomol. Chem.

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RSC - Org. Biomol. Chem. latest articles
Updated: 5 hours 17 min ago

Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,893-904
DOI: 10.1039/C4OB02238F, PaperPaolo Innocenti, Hannah Woodward, Lisa O'Fee, Swen Hoelder
A versatile and efficient entry into 2-amino-pyrido[3,4-d]pyrimidines was developed. Our strategy hinges on the concise preparation and derivatisation of 8-chloro-2-(methylthio)pyrido[3,4-d]pyrimidine intermediates to yield putative kinase inhibitors.
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Post-synthesis DNA modifications using a trans-cyclooctene click handle

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,909-915
DOI: 10.1039/C4OB02031F, PaperKe Wang, Danzhu Wang, Kaili Ji, Weixuan Chen, Yueqin Zheng, Chaofeng Dai, Binghe Wang
Efficient enzymatic DNA incorporation of trans-cyclooctene thymidine triphosphate (TCO-TTP) is reported. The general handle of trans-cyclooctene can undergo a rapid bioorthogonal cycloaddition with tetrazine, which is suitable for further DNA labeling work.
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A simple and robust preparation of N-acetylindoxyls: precursors for indigogenic substrates

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,905-908
DOI: 10.1039/C4OB02248C, PaperMichael N. Gandy, Lindsay T. Byrne, Keith A. Stubbs
A generalised, simple and efficient synthesis of N-acetyl-5-bromo-4-chloroindoxyl and related analogues required for the synthesis of indigogenic substrates to probe for biological activities is reported.
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New synthesis and biological evaluation of uniflorine A derivatives: towards specific insect trehalase inhibitors

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,886-892
DOI: 10.1039/C4OB02016B, PaperGiampiero D'Adamio, Antonella Sgambato, Matilde Forcella, Silvia Caccia, Camilla Parmeggiani, Morena Casartelli, Paolo Parenti, Davide Bini, Laura Cipolla, Paola Fusi, Francesca Cardona
(-)-Uniflorine A and 7-deoxy-uniflorine A are selective inhibitors of insect trehalases from C. riparius and S. littoralis.
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Transfer of antioxidants at the interfaces of model food emulsions: distributions and thermodynamic parameters

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,876-885
DOI: 10.1039/C4OB02058H, PaperSonia Losada-Barreiro, Veronica Sanchez-Paz, Carlos Bravo-Diaz
Caffeic acid and [small alpha]-tocopherol (vitamin E) incorporate spontaneously into the interfacial regions of emulsions and their transfer processes are entropy driven.
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Kinetic evaluation of glucose 1-phosphate analogues with a thymidylyltransferase using a continuous coupled enzyme assay

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,866-875
DOI: 10.1039/C4OB02057J, PaperS. M. Forget, A. Jee, D. A. Smithen, R. Jagdhane, S. Anjum, S. A. Beaton, D. R. J. Palmer, R. T. Syvitski, D. L. Jakeman
We have developed a continuous spectrophotometric kinetic assay for the detection of PPi and have applied the assay to evaluate Cps2L, a nucleotidylyltransferase, kinetics with five synthetic substrate analogues (2-6).
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A unified lead-oriented synthesis of over fifty molecular scaffolds

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,859-865
DOI: 10.1039/C4OB02287D, PaperRichard G. Doveston, Paolo Tosatti, Mark Dow, Daniel J. Foley, Ho Yin Li, Amanda J. Campbell, David House, Ian Churcher, Stephen P. Marsden, Adam Nelson
Sourcing large numbers of lead-like compounds is a major challenge; a unified synthetic approach enabled the efficient synthesis of 52 diverse lead-like molecular scaffolds from just 13 precursors.
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Synthesis of new unnatural N[small alpha]-Fmoc pyrimidin-4-one amino acids: use of the p-benzyloxybenzyloxy group as a pyrimidinone masking group

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,851-858
DOI: 10.1039/C4OB02235A, PaperAbdellatif ElMarrouni, Montserrat Heras
The p-benzyloxybenzyloxy group is used to mask the oxo function of the 4(3H)-pyrimidinone ring in the synthesis of new unnatural amino acids.
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A thermodynamic insight into the recognition of hydrophilic and hydrophobic amino acids in pure water by aza-scorpiand type receptors

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,843-850
DOI: 10.1039/C4OB02092H, PaperSalvador Blasco, Begona Verdejo, Carla Bazzicalupi, Antonio Bianchi, Claudia Giorgi, Concepcion Soriano, Enrique Garcia-Espana
Thermodynamic studies about the interaction of scorpiand aza-macrocycles with amino acids in water show entropy driven stabilisations often associated with solvation/desolvation processes.
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Sulfate recognition by a hexaaza cryptand receptor

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,834-842
DOI: 10.1039/C4OB02027H, PaperPedro Mateus, Rita Delgado, Vania Andre, M. Teresa Duarte
A polypyrrolic polyammonium macrobicycle encapsulates sulfate with very high association constants and selectivity in the presence of other anions.
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Synthesis of (phosphonomethyl)phosphinate pyrophosphate analogues via the phospha-Claisen condensation

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,825-833
DOI: 10.1039/C4OB02007C, PaperFabien Gelat, Claire Lacomme, Olivier Berger, Laurent Gavara, J.-L. Montchamp
Pyrophosphate analogues are of great importance especially for the design of biologically active molecules.
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Rapid synthesis of isoquinolinones by intramolecular coupling of amides and ketones

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,817-824
DOI: 10.1039/C4OB01948B, PaperWen-Tao Wei, Yu Liu, Lin-Miao Ye, Rong-Hui Lei, Xue-Jing Zhang, Ming Yan
Isoquinolinones were prepared in good yields via the intramolecular coupling of amides and ketones in the presence of KOt-Bu/DMF.
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Formation of the steroidal C-25 chiral center via the asymmetric alkylation methodology

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,776-782
DOI: 10.1039/C4OB02123A, PaperYu. V. Ermolovich, V. N. Zhabinskii, V. A. Khripach
A novel approach for the preparation of steroids containing a chiral center at C-25 is reported. The key stereochemistry inducing step was asymmetric alkylation of pseudoephenamine amides of steroidal C-26 acids. The developed methodology was successfully applied to the synthesis of (25R)- and (25S)-cholestenoic acids as well as (25R)- and (25S)-26-hydroxy brassinolides.
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Synthesis and the absolute configuration of both enantiomers of 4,5-dihydroxy-3-(formyl)cyclopent-2-enone acetonide as a new chiral building block for prostanoid synthesis

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,807-816
DOI: 10.1039/C4OB01535E, PaperBeata Lukasik, Marian Mikolajczyk, Grzegorz Bujacz, Remigiusz Zurawinski
Starting from optically inactive meso-tartaric acid (6) the synthesis of both enantiomers of a new cyclopentenone building block 5 was developed.
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A QSAR study on the inhibition mechanism of matrix metalloproteinase-12 by arylsulfone analogs based on molecular orbital calculations

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,793-806
DOI: 10.1039/C4OB01843E, PaperSeiji Hitaoka, Hiroshi Chuman, Kazunari Yoshizawa
The inhibition mechanism of matrix metalloproteinase-12 by arylsulfone analogs is revealed using a comprehensive computational approach including docking simulations, molecular orbital calculations, and QSAR.
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Interfacial catalysis of aldol reactions by prolinamide surfactants in reverse micelles

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,770-775
DOI: 10.1039/C4OB02074J, PaperPremkumar Rathinam Arivalagan, Yan Zhao
Aggregation of prolinamide surfactants in nonpolar solvents enhanced their catalytic activity and gave unusual substrate selectivity in aldol condensations.
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1,1-Alkenylboration of diarylphosphino-enynes: convenient synthetic entry to vicinal P/B Lewis pairs at extended conjugated [small pi]-frameworks

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,764-769
DOI: 10.1039/C4OB02134G, PaperGuo-Qiang Chen, Gerald Kehr, Constantin G. Daniliuc, Gerhard Erker
Alkenylboranes R-CH[double bond, length as m-dash]CH-B(C6F5)2 undergo carbon-carbon coupling by means of 1,1-alkenylboration with diarylphosphino-enynes to give conjugated hexatriene derivatives that bear a vicinal pair of B(C6F5)2 and PAr2 functionalities at the framework.
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Synthesis of functionalized 2-salicyloylfurans, furo[3,2-b]chromen-9-ones and 2-benzoyl-8H-thieno[2,3-b]indoles by one-pot cyclizations of 3-halochromones with [small beta]-ketoamides and 1,3-dihydroindole-2-thiones

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,729-750
DOI: 10.1039/C4OB01730G, PaperIryna Savych, Tim Glasel, Alexander Villinger, Vyacheslav Ya. Sosnovskikh, Viktor O. Iaroshenko, Peter Langer
Domino reactions of 3-halochromones with [small beta]-ketoamides and 1,3-dihydroindole-2-thiones provided a convenient approach to various heterocyclic systems.
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Exploiting the narrow gap of rearrangement between the substituents in the vicinal disubstitution reactions of diaryliodonium salts with pyridine N-sulfonamidates

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,751-763
DOI: 10.1039/C4OB01744G, PaperYong Wang, Ming Li, Lirong Wen, Peng Jing, Xiang Su, Chao Chen
The vicinal disubstitution reactions of diaryliodonium salts with pyridine N-sulfonamidates were studied fully to give o-pyridinium anilines.
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Irreversible covalent modification of type I dehydroquinase with a stable Schiff base

17 December, 2014 - 22:54

Org. Biomol. Chem., 2015, 13,706-716
DOI: 10.1039/C4OB01782J, PaperLorena Tizon, Maria Maneiro, Antonio Peon, Jose M. Otero, Emilio Lence, Sergio Poza, Mark J. van Raaij, Paul Thompson, Alastair R. Hawkins, Concepcion Gonzalez-Bello
Structural and computational studies carried out with two epoxides provide insight into the irreversible inhibition of type I dehydroquinase.
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