Org. and Biomol. Chem.

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RSC - Org. Biomol. Chem. latest articles
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Cu-Catalyzed arylation of amino group in the indazole ring: Regioselective synthesis of pyrazolo-carbazoles

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02044H, PaperK AnilKumar, Prakash Kannaboina, Devendra Kumar Dhaked, Ram A Vishwakarma, Prasad. V. Bharatam, Parthasarathi Das
Cu (II)-Catalyzed cross-coupling of various aryl boronic acids with 5 and 6-amino indazoles has resulted the (arylamino)-indazoles. These resulted (arylamino)-indazoles have been utilized in synthesizing medicinally important pyrazole fused-carbazoles via...
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Using Hansen solubility parameters to study the encapsulation of caffeine in MOFs

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB01898B, PaperLorena Paseta, Gregory Potier, Steven Abbott, Joaquin Coronas
Hansen solubility parameters (HSP) have found their greatest use in the evaluation of solvent-polymer chemical interactions. Given their great interest in the scientific community, host-guest interactions in metal-organic frameworks (MOFs),...
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Probing the target-specific inhibition of sensitized protein tyrosine phosphatases with biarsenical probes

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02256D, PaperAdam Pomorski, Justyna Adamczyk, Anthony Bishop, Artur Krezel
Selective control of enzyme activity is critical for elucidating the roles of specific proteins in signaling pathways. One potential means for developing truly target-specific inhibitors involves the use of protein...
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Unraveling the contributions of hydrogen-bonding interactions to the activity of native and non-native ligands in the quorum-sensing receptor LasR

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02252A, PaperJoseph P. Gerdt, Christine E. McInnis, Trevor L. Schell, Helen E. Blackwell
Quorum sensing (QS) via the synthesis and detection of N-acyl L-homoserine lactone (AHL) signals regulates important pathogenic and mutualistic phenotypes in many bacteria. Over the past two decades, the development...
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Reactivity of aldehydes at the Air-Water Interface. Insights from molecular dynamics simulations and ab initio calculations.

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02029D, PaperMarilia T.C. Martins-Costa, Francisco F. Garcia-Prieto, Manuel F. Ruiz-Lopez
Understanding the influence of solute-solvent interactions on chemical reactivity has been a subject of intense research in the last decades. Theoretical studies have focused on bulk solvation phenomena and a...
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Vertically-expanded imidazo[1,2-a]pyridines and imidazo[1,5-a]pyridine via dehydrogenative coupling

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02383H, PaperDaniel Gryko, Marzena Banasiewicz, Dikhi Firmansyah
Anion-radical coupling of structurally diverse series of aromatic compounds possessing biaryl linkages led to seven fused, polycyclic heterocycles in reasonable yields. The yield of the key step (K, toluene, O2)...
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Domino Reaction Involving the Bestmann-Ohira Reagent and [small alpha],[small beta]-Unsaturated Aldehydes: Efficient Synthesis of functionalized pyrazoles

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02365J, PaperShakir Ahamad, Ashis Kumar Gupta, Ruchir Kant, Kishor Mohanan
A mild, efficient and rapid domino reaction involving the Bestmann-Ohira reagent (BOR) and [small alpha],[small beta]-unsaturated aldehydes has been developed for the synthesis of densely functionalized vinylpyrazoles. This reaction demonstrates the dual...
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Regioselective synthesis, antimicrobial evaluation and theoretical studies of 2-styryl quinolines

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02277G, PaperAhmed Kamal, Rahim Abdul, Sd Riyaz, Poornachandra Y, Balakrishna Moku, Ganesh Kumar C., Ali S. M. Hussaini, Sridhar Balasubramanian, Pavan Kumar Machiraju
2-Styryl quinolines (9a-l) have been synthesized regioselectively from 2-methyl-quinoline by using NaOAc in water acetic acid binary solvents and evaluated for their antibacterial activity against both Gram-positive and Gram-negative strains....
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Development of an efficient route to CF3-substituted pyrrolopyrimidines through understanding the competition between Michael and nitro-Mannich reactions

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02233E, PaperValentine Nenajdenko, M Vovk, Volodymyr Andriyovych Sukach, Viktor Mykolayovych Tkachuk, K Kovalchuk
Regioselective base-catalyzed addition of nitromethane to 2-oxo-4-trifluoromethyl-1,2-dihydropyrimidine-5-carboxylates is reported. It was found that Michael-like pathway is highly reversible and substantially dominating under conditions of kinetic control (0-5 [degree]C, 10 h)...
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The synthesis of head-to-tail cyclic sulfono-[gamma]-AApeptides

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02232G, CommunicationHaifan Wu, Fengyu She, Wenyang Gao, Austin Prince, Yaqiong Li, Lulu Wei, Allison Mercer, Lukasz Wojtas, Shengqian Ma, Jianfeng Cai
Head-to-tail cyclic sulfono-[gamma]-AApeptides.
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Direct oxidative coupling of thiols and benzylic ethers via C(sp3)-H activation and C-O cleavage to lead thioesters

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02250E, CommunicationJ. Feng, M.-F. Lv, G.-P. Lu, C. Cai
An unprecedented protocol for the synthesis of thioesters via C-H thioesterification and C-O cleavage was developed. This CDC protocol was found convenient and easy-to-handle involving the use of DTBP as the only green oxidant.
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The synthesis of [18F]pitavastatin as a tracer for hOATP using the Suzuki coupling

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01953A, PaperYusuke Yagi, Hiroyuki Kimura, Kenji Arimitsu, Masahiro Ono, Kazuya Maeda, Hiroyuki Kusuhara, Tetsuya Kajimoto, Yuichi Sugiyama, Hideo Saji
Fluorine-18 labeled radiotracers, such as [18F]fluorodeoxyglucose, can be used as practical diagnostic agents in positron emission tomography (PET).
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The development of a complementary pathway for the synthesis of aliskiren

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01963F, PaperLe-Le Li, Jin-Ying Ding, Lian-Xun Gao, Fu-She Han
We present an alternative pathway for the synthesis of aliskiren by applying the Evans chiral auxiliary-aided asymmetric allylation and the Julia-Kocienski olefination as the key transformations.
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Cationic dialkylarylphosphates: a new family of bio-inspired cationic lipids for gene delivery

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01770F, PaperStephanie S. Le Corre, Nawal Belmadi, Mathieu Berchel, Tony Le Gall, Jean-Pierre Haelters, Pierre Lehn, Tristan Montier, Paul-Alain Jaffres
The synthesis of mono- and di-cationic lipophosphates is reported. These cationic lipids were formulated as liposomal solutions, and their capacity to transfect cells was evaluated on three cell lines.
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Synthesis and antitumor activity of novel 2-substituted indoline imidazolium salt derivatives

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02385D, PaperXiao-Liang Xu, Chun-Lei Yu, Wen Chen, Ying-Chao Li, Li-Juan Yang, Yan Li, Hong-Bin Zhang, Xiao-Dong Yang
A series of novel 2-substituted indoline imidazolium salt derivatives has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence...
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Investigation of the Passerini and Ugi Reactions in [small beta]-Lactam Aldehydes. Synthetic Applications

25 November, 2014 - 17:17
Org. Biomol. Chem., 2014, Accepted Manuscript
DOI: 10.1039/C4OB02289K, PaperBenito Alcaide, Pedro Almendros, Cristina Aragoncillo, Ricardo Callejo, Maria Pilar Ruiz, M. Rosario Torres
Passerini (P-3CR) and Ugi (U-4CR) reactions were investigated in 4-oxoazetidine-2-carboxaldehydes affording the corresponding Passerini and Ugi adducts with moderate diastereoselectivity in high yields. Fortunately, the obtained mixtures of isomers syn/anti...
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Bioorthogonal labelling of 3-nitrotyrosine in peptides and proteins through diazotisation mediated azidation

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB02133A, CommunicationJohn Y. Ng, Jason W. H. Wong
A bioorthogonal method of transforming 3-nitrotyrosine to 3-azidotyrosine is described, providing new opportunities to study 3-nitrotyrosine in biological samples.
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Bleomycin-induced trans lipid formation in cell membranes and in liposome models

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01924E, PaperAysegul Cort, Tomris Ozben, Anna Sansone, Sebastian Barata-Vallejo, Chryssostomos Chatgilialoglu, Carla Ferreri
Bleomycin-iron complexes cause lipid cis-trans isomerisation through thiyl radical formation and reactivity with unsaturated phospholipids, revealing membranes as a relevant and novel site of drug effect.
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Determination of the absolute configuration of phosphinic analogues of glutamate

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01960A, PaperBruno Commare, Delphine Rigault, Isabelle A. Lemasson, Patrick Deschamps, Alain Tomas, Pascal Roussel, Isabelle Brabet, Cyril Goudet, Jean-Philippe Pin, Frederic R. Leroux, Francoise Colobert, Francine C. Acher
Stereomers of LSP1-2111 have been separated, their absolute configuration and agonist activity at mGlu4R determined.
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Anionic glycolipids related to glucuronosyldiacylglycerol inhibit protein kinase Akt

25 November, 2014 - 17:17

Org. Biomol. Chem., 2015, Advance Article
DOI: 10.1039/C4OB01602E, PaperMaria Vetro, Barbara Costa, Giulia Donvito, Noemi Arrighetti, Laura Cipolla, Paola Perego, Federica Compostella, Fiamma Ronchetti, Diego Colombo
Long chain GlcADG analogues synthesized as PI3P mimics inhibited isolated Akt and proliferation of human ovarian carcinoma IGROV-1 cells.
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