Archive for the ‘Hot articles’ Category

Vaccines for heroin

The number of deaths due to heroin overdoses has severely increased in last decade, and regular consumption of heroin leads to serious health concerns.

Vaccination is one of the emerging choices among heroin rehabilitation therapies. In general, these vaccines contain heroin-like hapten as a pharmacophore that acts as an antagonist. This antagonist has high affinity for heroin receptors but does not activate them, hence reverses the effects of heroin. Because of inherent chemical instability, when entered in to bloodstream these anti-heroin drugs rapidly metabolise into several by-products, which makes development of effective vaccines against heroin particularly challenging.

Recently an American research group at National Institute on Drug Abuse (NIDA) lead by Professor Kenner Rice has reported the synthesis and immunological evaluation for a series of haptens.

The team has emphasised the hydrolytic stability of hapten scaffolds and envisioned that hapten with amido groups at both the C3 and C6 positions should be more stable than a hapten with an ester in one of those positions. Insertion of a 3-amino group and the construction of a C-6α-(2-oxo-propyl) group stereoselectively was the challenging task towards the synthesis of designed hapten derivatives. The group has tackled the synthetic hurdle by adopting convergent synthesis approach and validating the stereochemistry by single X ray crystallography.

Furthermore, in vivo Immunological studies of all three new synthetic haptens reveals that one derivative DiAmHap (3) is chemically more stable and better candidate for a heroin vaccine than 6-PrOxyHap (1) and DiPrOxyHap (2). This work is a very positive step towards the development of vaccines for heroin abuse.

Synthesis and immunological effects of heroin vaccines
Fuying Li, Kejun Cheng,  Joshua F. G. Antoline, Malliga R. Iyer, Gary R. Matyas, Oscar B. Torres, Rashmi Jalah, Zoltan Beck, Carl R. Alving, Damon A. Parrish, Jeffrey R. Deschamps, Arthur E. Jacobson and Kenner C. Rice
DOI: 10.1039/C4OB01053A

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Recent HOT Organic & Biomolecular Chemistry articles

Check out the following HOT articles, these have been made free to access for a limited time:

Synthesis and immunological effects of heroin vaccines
Fuying Li, Kejun Cheng, Joshua F. G. Antoline, Malliga R. Iyer, Gary R. Matyas, Oscar B. Torres, Rashmi Jalah, Zoltan Beck, Carl R. Alving, Damon A. Parrish, Jeffrey R. Deschamps, Arthur E. Jacobson and Kenner C. Rice
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB01053A

Synthesis and immunological effects of heroin vaccines

Free to access until 21st August 2014


6-Azido hyacinthacine A2 gives a straightforward access to the first multivalent pyrrolizidine architectures
Giampiero D’Adamio, Camilla Parmeggiani, Andrea Goti, Antonio J. Moreno-Vargas, Elena Moreno-Clavijo, Inmaculada Robina and Francesca Cardona
Org. Biomol. Chem., 2014,12, 6250-6266
DOI: 10.1039/C4OB01117A

6-Azido hyacinthacine A2 gives a straightforward access to the first multivalent pyrrolizidine architectures

Free to access until 21st August 2014


Relative contractile motion of the rings in a switchable palindromic [3]rotaxane in aqueous solution driven by radical-pairing interactions
Leah S. Witus, Karel J. Hartlieb, Yuping Wang, Aleksandrs Prokofjevs, Marco Frasconi, Jonathan C. Barnes, Edward J. Dale, Albert C. Fahrenbach and J. Fraser Stoddart
Org. Biomol. Chem., 2014,12, 6089-6093
DOI: 10.1039/C4OB01228C

Relative contractile motion of the rings in a switchable palindromic [3]rotaxane in aqueous solution driven by radical-pairing interactions

Free to access until 21st August 2014


Catalytic control over the formation of supramolecular materials
Rienk Eelkema and Jan H. van Esch
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB01108B

Catalytic control over the formation of supramolecular materials

Free to access until 21st August 2014


Comparison of the substrate selectivity and biochemical properties of human and bacterial γ-butyrobetaine hydroxylase
Anna M. Rydzik, Ivanhoe K. H. Leung, Grazyna T. Kochan, Nikita D. Loik, Luc Henry, Michael A. McDonough, Timothy D. W. Claridge and Christopher J. Schofield
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB01167H

Comparison of the substrate selectivity and biochemical properties of human and bacterial γ-butyrobetaine hydroxylase

Free to access until 21st August 2014


Diaporine, a novel endophyte-derived regulator of macrophage differentiation
Hao Chen Wu, Hui Ming Ge, Le Yun Zang, Yun Cheng Bei, Zhi Yuan Niu, Wei Wei, Xiu Jing Feng, Sen Ding, Seik Weng Ng, Ping Ping Shen and Ren Xiang Tan
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB01123F

Diaporine, a novel endophyte-derived regulator of macrophage differentiation

Free to access until 21st August 2014


New reagents for detecting free radicals and oxidative stress
Mina Barzegar Amiri Olia, Carl H. Schiesser and Michelle K. Taylor
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB01172D

New reagents for detecting free radicals and oxidative stress

Free to access until 21st August 2014

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Recent HOT Organic & Biomolecular Chemistry articles

Enantioselective synthesis of spiroacetals: the conquest of a long-sought goal in asymmetric catalysis
Lara Cala, Francisco J. Fañanás and Félix Rodríguez  
Org. Biomol. Chem., 2014,12, 5324-5330
DOI: 10.1039/C4OB00737A

Enantioselective synthesis of spiroacetals: the conquest of a long-sought goal in asymmetric catalysis

Free to access until 1st August 2014


Multivalent glycosylated nanoparticles for studying carbohydrate–protein interactions
Avijit K. Adak, Hong-Jyune Lin and Chun-Cheng Lin
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB00827H

Multivalent glycosylated nanoparticles for studying carbohydrate–protein interactions

Free to access until 1st August 2014


A simple approach to pyrrolylimidazole derivatives by azirine ring expansion with imidazolium ylides
Alexander F. Khlebnikov, Olesya A. Tomashenko, Liya D. Funt and Mikhail S. Novikov  
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB00865K

A simple approach to pyrrolylimidazole derivatives by azirine ring expansion with imidazolium ylides

Free to access until 1st August 2014


Enantioselective palladium catalyzed conjugate additions of ortho-substituted arylboronic acids to β,β-disubstituted cyclic enones: total synthesis of herbertenediol, enokipodin A and enokipodin B
Jeffrey Buter, Renée Moezelaar and Adriaan J. Minnaard  
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB01085J

Enantioselective palladium catalyzed conjugate additions of ortho-substituted arylboronic acids to β,β-disubstituted cyclic enones: total synthesis of herbertenediol, enokipodin A and enokipodin B

Free to access until 1st August 2014


Conversion of S-phenylsulfonylcysteine residues to mixed disulfides at pH 4.0: utility in protein thiol blocking and in protein-S-nitrosothiol detection
B. D. Reeves, N. Joshi, G. C. Campanello, J. K. Hilmer, L. Chetia, J. A. Vance, J. N. Reinschmidt, C. G. Miller, D. P. Giedroc, E. A. Dratz, D. J. Singel and P. A. Grieco  
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB00995A

Conversion of S-phenylsulfonylcysteine residues to mixed disulfides at pH 4.0: utility in protein thiol blocking and in protein-S-nitrosothiol detection

Free to access until 1st August 2014


A tryptophan responsive fluorescent and wettable dual-signal switch
Xiaoyan Zhang, Jing Li, Ningmei Feng, Li Luo, Zhen Dai, Li Yang, Demei Tian and Haibing Li
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB00792A

A tryptophan responsive fluorescent and wettable dual-signal switch

Free to access until 1st August 2014

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When a Spectator is not Just a Spectator in Iodonium Salts

Advances in hypervalent iodine are flourishing1 from the classic non-toxic Dess-Martin periodinane oxidation to synthetic reagents for elaborate natural products2. New types of both iodine(III) and iodine(V) compounds are constantly being discovered for ever increasing applications.

Iodonium salts, classified as iodine(III) compounds, are notoriously electrophilic. Those with two carbon ligands like alkynyl(aryl)iodonium salts react with a nucleophile which couples with the alkyne.  Overall, the reaction seemingly pieces together two nucleophilic entities.

The remaining aryl iodide in the balanced equation seems to be a “spectator” since it is absent in the product, but in this recent (open access) paper Hamnett and Moran sought to investigate whether that is truly the case.

They improved the preparation of alkynyl(aryl)iodonium tosylates and systematically applied them to two model reactions, finding that the 2-anisyl ligand provided the highest yields.

It significantly out-performed the 3-anisyl derivative, suggesting that the key to success is the inherent stability of the 2-anisyl iodonium salt with the methoxy group ideally situated for coordination to the iodine.

Discovering the effectiveness of the 2-anisyl ligand in iodonium salts could have implications for more efficient transformations involving hypervalent iodine.  More broadly, the work shows the importance of optimizing reactions across all variables and highlighting that spectators may not always be simple bystanders.

To find out more see:

Improving alkynyl(aryl)iodonium salts: 2-anisyl as a superior aryl group
David J. Hamnett and Wesley J. Moran
DOI: 10.1039/C4OB00556B


1. M. S. Yusubov, A. V. Maskaev and V. V. Zhdankin, ARKIVOC, 2011, i, 370–409.
2. D. J. Wardrop and J. Fritz, Org. Lett., 2006, 8, 3659–3662.

Posted on behalf of Jennifer Lee, guest web writer for Organic & Biomolecular Chemistry

Jennifer LeeJennifer Lee is currently a Ph.D. candidate in Dr. George Kraus’ organic chemistry lab at Iowa State University. Her research focuses on designing methodologies to transform carbohydrate-derived biomass into biorenewable commodity and specialty chemicals. The creation of a versatile platform technology led to diverse and industrially-relevant aromatic compounds to work toward a more sustainable future.

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Polyamine modification by acrolein exclusively produces 1,5-diazacyclooctanes: a previously unrecognized mechanism for acrolein-mediated oxidative stress
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Evaluation of 4-substituted styrenes as functional monomers for the synthesis of theophylline-specific molecularly imprinted polymers
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In(OTf)3-catalysed one-pot versatile pyrrole synthesis through domino annulation of α-oxoketene-N,S-acetals with nitroolefins
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In(OTf)3-catalysed one-pot versatile pyrrole synthesis through domino annulation of α-oxoketene-N,S-acetals with nitroolefins

 

Free to access until 18th July 2014


Improving alkynyl(aryl)iodonium salts: 2-anisyl as a superior aryl group
David J. Hamnett and Wesley J. Moran  
Org. Biomol. Chem., 2014,12, 4156-4162
DOI: 10.1039/C4OB00556B

Graphical abstract

Free to access until 4th July 2014


Recent development of two-photon fluorescent probes for bioimaging
Dokyoung Kim, Hye Gun Ryu and Kyo Han Ahn
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB00431K

Graphical abstract

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A succinyl lysine-based photo-cross-linking peptide probe for Sirtuin 5
Karunakaran A. Kalesh and Edward W. Tate  
Org. Biomol. Chem., 2014,12, 4310-4313
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Marine bacteria from the Roseobacter clade produce sulfur volatiles via amino acid and dimethylsulfoniopropionate catabolism
Nelson L. Brock, Markus Menke, Tim A. Klapschinski and Jeroen S. Dickschat  
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Hydrogen bond directed epoxidation: diastereoselective olefinic oxidation of allylic alcohols and amines
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Org. Biomol. Chem., 2014, Advance Article
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An intracellularly activatable, fluorogenic probe for cancer imaging
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Org. Biomol. Chem., 2014, Advance Article
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Palladium mediated intramolecular multiple C–X/C–H cross coupling and C–H activation: synthesis of carbazole alkaloids calothrixin B and murrayaquinone A
Srinivasan A. Kaliyaperumal, Shyamapada Banerjee and Syam Kumar U. K.
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C4OB00493K

Graphical abstract

Free to access until 4th July 2014

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Cyclodextrin ion channels
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HOT Organic & Biomolecular Chemistry articles for March – updated throughout the month

A computational and experimental study of O-glycosylation. Catalysis by human UDP-GalNAc polypeptide:GalNAc transferase-T2
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Out-Basicity of 1,8-bis(dimethylamino)naphthalene: the experimental and theoretical challenge
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Carboxy-directed asymmetric hydrogenation of α-alkyl-α-aryl terminal olefins: highly enantioselective and chemoselective access to a chiral benzylmethyl center
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Org. Biomol. Chem., DOI: 10.1039/C4OB00018H, Communication
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Chromane helicity rule – scope and challenges based on an ECD study of various trolox derivatives
Marcin Górecki, Agata Suszczyńska, Magdalena Woźnica, Aneta Baj, Michał Wolniak, Michał K. Cyrański, Stanisław Witkowski and Jadwiga Frelek
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Reaction pathways and free energy profiles for cholinesterase-catalyzed hydrolysis of 6-monoacetylmorphine
Yan Qiao, Keli Han and Chang-Guo Zhan
Org. Biomol. Chem., DOI: 10.1039/C3OB42464B, Paper
Free to access until 10th April

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HOT Organic & Biomolecular Chemistry articles for February

Synthetic strategies toward hetidine and hetisine-type diterpenoid alkaloids
Amy M. Hamlin, Jessica K. Kisunzu and Richmond Sarpong
Org. Biomol. Chem., 2014, DOI: 10.1039/C3OB42541J

Free to access until 28th March


Oxenoids in organic synthesis
Yury Minko and Ilan Marek
Org. Biomol. Chem., 2014, DOI: 10.1039/C3OB42349B

Free to access until: 17th March 2014

 Oxenoids in organic synthesis


A concise formation of N-substituted 3,4-diarylpyrroles – synthesis and cytotoxic activity
Maxim Egorov, Bernard Delpech, Geneviève Aubert, Thierry Cresteil, Maria Concepcion Garcia-Alvarez, Pascal Collin and Christian Marazano
Org. Biomol. Chem., 2014, DOI: 10.1039/C3OB42309C

Free to access until: 17th March 2014

synthesis of N-substituted 3,4-diarylpyrroles


Enantioselective synthesis of α-halo-α-alkylmalonates via phase-transfer catalytic α-alkylation
Suckchang Hong, Minsik Kim, Myunggi Jung, Min Woo Ha, Myungmo Lee, Yohan Park, Mi-hyun Kim, Taek-Soo Kim, Jihoon Lee and Hyeung-geun Park
Org. Biomol. Chem., 2014, DOI: 10.1039/C3OB42107D

Free to access until: 17th March 2014

Enantioselective synthesis of α-halo-α-alkylmalonates via phase-transfer catalytic α-alkylation

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HOT Organic & Biomolecular Chemistry articles for January

A highly selective chemodosimeter for fast detection and intracellular imaging of Hg2+ ions based on a dithiocarbamate–isothiocyanate conversion in aqueous ethanol
Suman Pal, Joydev Hatai, Mousumi Samanta, Alok Shaurya and Subhajit Bandyopadhyay  
Org. Biomol. Chem., 2014,12, 1072-1078
DOI: 10.1039/C3OB42108B

 Graphical abstract


Ethynylbenzenoid metabolites of Antrodia camphorata: synthesis and inhibition of TNF expression
Marco Buccini, Kathryn A. Punch, Belinda Kaskow, Gavin R. Flematti, Brian W. Skelton, Lawrence J. Abraham and Matthew J. Piggott  
Org. Biomol. Chem., 2014,12, 1100-1113
DOI: 10.1039/C3OB42333F

Free to access until 21st February 2014

Graphical abstract


Hypervalent iodine(III)-mediated cyclopropa(e)nation of alkenes/alkynes under mild conditions
Shaoxia Lin, Mengru Li, Zhiyong Dong, Fushun Liang and Jingping Zhang  
Org. Biomol. Chem., 2014, Advance Article
DOI: 10.1039/C3OB42123F

Free to access until 21st February 2014

Graphical abstract

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HOT Organic & Biomolecular Chemistry articles for December

Chiral amides via copper-catalysed enantioselective conjugate addition
Anne K. Schoonen, M. Ángeles Fernández-Ibáñez, Martín Fañanás-Mastral, Johannes F. Teichert and Ben L. Feringa  
Org. Biomol. Chem., 2014,12, 36-41, DOI: 10.1039/C3OB41923A 

Free to access until 16th January 2014

Chiral amides via copper-catalysed enantioselective conjugate addition

  


 Acylthioureas as anion transporters: the effect of intramolecular hydrogen bonding
Cally J. E. Haynes, Nathalie Busschaert, Isabelle L. Kirby, Julie Herniman, Mark E. Light, Neil J. Wells, Igor Marques, Vítor Félix and Philip A. Gale  
Org. Biomol. Chem., 2014,12, 62-72, DOI: 10.1039/C3OB41522H 

Free to access until 16th January 2014

Acylthioureas as anion transporters: the effect of intramolecular hydrogen bonding

  


 

Synthesis of substituted pyrenes by indirect methods
Juan M. Casas-Solvas, Joshua D. Howgego and Anthony P. Davis  
Org. Biomol. Chem., 2014,12, 212-232, DOI: 10.1039/C3OB41993B   

Free to access until 16th January 2014

Synthesis of substituted pyrenes by indirect methods

  

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