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Organic & Biomolecular Chemistry

Rapid publication of high quality organic chemistry research
Impact Factor 3.562 48 Issues per Year Indexed in Medline
 
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Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00899B, Paper
Abstract Stable-isotope-labeled precursors were used to establish the biosynthetic pathway leading from -alanine towards isoxazolin-5-one glucoside 1 and its 3-nitropropanoate (3-NPA) ester 2 in Chrysomelina larvae. Both structural elements originate...
 
Margaret A Brimble, Zaid Amso, Renata Kowalczyk, Young-Eon Park, Maureen Watson, Jian-Ming Lin, David Musson and Jill Cornish
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00983B, Paper
From themed collection Selective Chemistry with Peptides and Proteins
The cyclohexapeptide natural product dianthin G promotes osteoblast (bone-forming cell) proliferation in vitro at nanomolar concentrations, and is therefore considered a promising candidate for the treatment of osteoporosis. An Nα-methyl...
 
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00870D, Paper
Counterion competitive complexation is a background process currently ignored by using ionic host. Consequently guest binding constants are strongly affected by the design of the titration experiments in such a...
 
Bing Yang, Xiaozhou Ji, Yunsheng Xue, Haowei Zhang, Minxing Shen, Bo Jiang and Guigen Li
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00847J, Paper
A series of aza-Morita–Baylis–Hillman acrylates have been synthesized by using chiral N-phosphonyl imines and GAP chemistry/technology.
 
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB01038E, Paper
The synthesis of β,β-diaryl aryl propiophenones have been realized via palladium-catalyzed domino reactions of dimethyl amino functionalized enaminones and aryl boronic acids. This is the first example of transition metal-catalyzed...
 
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB01083K, Communication
A novel method for the preparation of 2-carboxyl-3-aryl quinoline derivatives from anilines, ethyl glyoxalate and enol ethers as phenylacetaldehyde surrogates is reported. The three-component coupling reaction occurs rapidly under mild...
 
Niall A. Anderson, Ian B. Campbell, Brendan J. Fallon, Sean M. Lynn, Simon J. F. Macdonald, John M. Pritchard, Panayiotis A. Procopiou, Steven L. Sollis and Lee R. Thorp
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00496B, Paper
Integrin inhibitor (cell adhesion assays) pIC50 αvβ6 = 8.4, αvβ3 = 6.0, αvβ5 = 5.9 and αvβ8 = 7.7.
 
Neal Dalton, Christopher P. Gordon, Timothy P. Boyle, Nicholas Vandegraaf, John Deadman, David I. Rhodes, Jonathan A. Coates, Stephen G. Pyne, Paul A. Keller and John B. Bremner
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00950F, Paper
From library screening of synthetic antimicrobial peptides, an O-allyltyrosine-based tripeptide HIV-1 integrase (IN) inhibitor was identified. Subsequent optimisation afforded an analogue exhibiting an IC50 value of 2.5 μM.
 
Jian-Siang Poh, Cristina García-Ruiz, Andrea Zúñiga, Francesca Meroni, David C. Blakemore, Duncan L. Browne and Steven V. Ley
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00970K, Paper
From themed collection Contemporary Synthetic Chemistry in Drug Discovery
We report conditions for the preparation of a range of trifluoromethylated isoxazole building blocks through the cycloaddition reaction of trifluoromethyl nitrile oxide and their subsequent derivatisation.
 
Ya-Dong Wu, Bei Huang, Yue-Xin Zhang, Xiao-Xu Wang, Jian-Jun Dai, Jun Xu and Hua-Jian Xu
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00876C, Communication
The KI-catalyzed reaction of acetone with aromatic carboxylic acids is achieved, leading to α-acyloxycarbonyl compounds in good to excellent yields under mild reaction conditions. The present method exhibits good functional-group...
 
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C5OB02339D, Communication
We discovered in the current study that six side chain-to-side chain cyclic pentapeptides harboring a central N(epsilon)-dodecyl (or tetradecyl)-thiocarbamoyl-lysine residue all behaved as highly potent (nM level) inhibitors against human...
 
Sandeep Thanna, Susan E Knudson, Anna Grezegorzewic, Sunayana Kapil, Christopher M Goins, Donald R Ronning, Mary Jackson, Richard A Slayden and Steven Joseph Sucheck
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00821F, Paper
Tuberculosis (TB) and its drug resistant forms kills more people than any other infectious disease. This fact emphasizes the need to identify new drugs to treat TB. 2-Aminothiophenes (2AT) have...
 
Elisabetta Rossi, Giorgio Abbiati, Monica Dell'Acqua, Marco Negrato, Andrea Paganoni and Valentina Pirovano
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00672H, Paper
A study on the SN2-type ring opening reactions of aziridines with indoles as nucleophiles is reported. Under gold(I) catalysis a great variety of tryptamine derivatives were prepared in good to...
 
Sami Marroun, Sabine Montaut, Stephanie Marques, Pierre Lafite, Gael Coadou, Patrick Rollin, guillaume Jousset, marie schuler, Arnaud Tatibouet, Hassan Oulyadi and Richard Daniellou
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB01003B, Paper
Thioglycosides, even if rare in Nature, have gained increased interests for their biological properties. Chemical syntheses of this class of compounds have been largely studied but little has been reported...
 
Ning Zhao, Sunting Xuan, Brandon Byrd, Frank R Fronczek, Kevin M Smith and M Graca H Vicente
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00935B, Communication
Three perhalogenated BODIPYs (1b-3b), bearing chloro and bromo groups at all carbon positions, were synthesized and characterized. The reactivity of BODIPY 3b was investigated under Stille cross-coupling reactions, and single...
 
Joseph Tillotson, Bharat P. Bashyal, MinJin Kang, Taoda Shi, Fabian De La Cruz, A. A. Leslie Gunatilaka and Eli Chapman
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00560H, Communication
Through the addition of chlorine atoms to the aromatic ring of 10(11)-dehydrocurvularin, covalent inhibition was tuned for p97 selectivity relative to the proteasome.
 
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00748A, Paper
This study allows the proposal of new mechanistic concepts that considerably change and improve our understanding of the reaction pathway.
 
Xuan Fu, Lili Lin, Yong Xia, Pengfei Zhou, Xiaohua Liu and Xiaoming Feng
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00948D, Communication
A highly diastereo- and enantioselective [3 + 3] annulation of donor–acceptor cyclopropanes with mercaptoacetaldehyde has been developed.
 
Masatoshi Shibuya, Masanori Abe, Shoji Fujita and Yoshihiko Yamamoto
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00900J, Paper
PhSiH3–I2 and PhSiH3–NIS generate PhSiH2I as a possible active species and cause diverse transformations.
 
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00825A, Communication
Mild and efficient synthesis of benzophenones via Ir(III)- and Rh(III)-catalyzed, directing group-assisted formyl C–H arylation of benzaldehydes has been achieved using diaryliodonium salts, in which Rh(III) and Ir(III) catalysts exhibited a complementary substrate scope.
 
Charlotte Vranken, Andrea Fin, Peter Tufar, Johan Hofkens, Michael Burkart and Yitzhak Tor
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00844E, Communication
SalL, an enzyme that catalyzes the synthesis of SAM from L-methionine and 5’-chloro-5’-deoxyoadenosine, is shown to accept 5’-chloro-5’-deoxythienoadenosine as a substrate and facilitate the synthesis of a synthetic SAM analog...
 
Bianka Söveges, Tímea Imre, Tamás Szende, Ádám Levente Póti, Gergely Balázs Cserép, Tamas Hegedus, Peter Kele and Krisztina Németh
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00810K, Paper
Fluorescent tagging of proteins via accessible cysteine residues is of paramount importance. In this study, model proteins of interest (mitogen-activated protein kinases) were labeled successfully in native state on their...
 
Trieu Trinh, Eileen A McLaughlin, Mohammed Abdel-Hamid, Christopher Gordon, liana Bernstein, Victoria Aye, Peter Cossar, Jennette Sakoff and Adam McCluskey
Org. Biomol. Chem., 2016, Accepted Manuscript
DOI: 10.1039/C6OB00606J, Paper
A series of quinolone-2-(1H)-ones from the Ugi-Knoevenagel three- and four- component reaction were prepared exhibiting low micromolar cytotoxicity against a panel of eight human cancer cell lines known to possess...
 
Hua Xu, Ariamala Gopalsamy, Erik C. Hett, Shores Salter, Ann Aulabaugh, Robert E. Kyne, Betsy Pierce and Lyn H. Jones
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB01078D, Communication
Proof of drug-target engagement in physiologically-relevant contexts is a key pillar of successful therapeutic target validation.
 
Org. Biomol. Chem., 2016, Advance Article
DOI: 10.1039/C6OB00814C, Communication
From themed collection Contemporary Synthetic Chemistry in Drug Discovery
An organocatalytic formal [4 + 2] cycloaddition reaction has been developed that permits rapid access to bicyclo[2.2.1]heptane-1-carboxylates with excellent enantioselectivities under mild and operationally simple conditions.
 
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