Nominations for the 2012 RSC Prizes and Awards close on the 15 January 2012
Our Prizes and Awards represent the dedication and outstanding achievements and are a platform to showcase inspiring science to gain the recognition deserved. Don’t forget to nominate colleagues who have made a significant contribution to advancing the chemical sciences.
View our full list of Prizes and Awards and use the online system to nominate a colleague.
Welcome to the final issue of 2011!
On the outside front cover of this issue is an article from Chang-Sik Ha and coworkers on a one step synthetic route to a hierarchical mesoporous bio-polymer/silica composite material with bimodal mesopores using a dual template of N,N,N-trimethyl chitosan (TMCs) and sodium dodecyl sulfate (SDS) for pH-sensitive targeted drug release.
Hierarchical mesoporous bio-polymer/silica composites co-templated by trimethyl chitosan and a surfactant for controlled drug delivery
Vijay Kumar Rana, Sung Soo Park, Surendran Parambadath, Mi Ju Kim, Sun-Hee Kim, Satyendra Mishra, Raj Pal Singh and Chang-Sik Ha
DOI: 10.1039/C0MD00222D
On the inside front cover Adrian Schwan et al. report a a novel phospholipase-resistant C16:0, C16:1 diether phosphonoglycerol as a synthetic lung surfactant with surface activity equivalent to calf lung surfactant extract.
Synthesis and activity of a novel diether phosphonoglycerol in phospholipase-resistant synthetic lipid:peptide lung surfactants
Adrian L. Schwan, Suneel P. Singh, Jason A. Davy, Alan J. Waring, Larry M. Gordon, Frans J. Walther, Zhengdong Wang and Robert H. Notter
DOI: 10.1039/C1MD00206F
As with all our cover articles these are free to access for 6 weeks.
View the rest of the issue here
On behalf of Professor Dr Koen Augustyns (University of Antwerp), Guest Editor, we would like to invite authors to contribute to this themed issue which aims collect together in one place some of the latest exciting research from across the breadth of drug residence and covalent drug research.
Analysis of drug-target residence time has begun to play a larger role in drug discovery as suggested by recent literature. For compounds with a slow off rate, long action at the target may render a perfect pharmacokinetic profile unnecessary, and selectivity vs. other targets inhibited only briefly may be more readily achieved. Reversible and irreversible covalent binding drugs may be considered as the logical extreme for this approach. For other targets or therapeutic areas, other kinetic profiles may be desirable. Finally, there is a real need to build a better understanding in the medicinal chemistry community of the preferred profiles, screening methods, at which stage of a project lifetime to characterize the kinetics, and ideally a structural bases for design to achieve a desired kinetic profile.
-Koen Augustyns, Guest Editor
Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work. In addition, as this is a web-based theme issue, printing of articles will not be held for a specific issue thereby allowing rapid dissemination of the science presented online and in print without delay. Both reviews and primary research are suitable for this issue.
The submission deadline for the web theme issue will be Monday 6th February 2012.
If you would like to contribute to this exciting themed issue, please contact the Editorial Office.
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Free online access to MedChemComm will finish at the end of 2011, but there is still time to take a look at all the articles we’ve published so far free of charge. Don’t know where to start? Why not take a look at some of the top accessed articles over the last year: |
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Molecular obesity is weighing down drug discovery Michael Hann from GSK suggests that the search for potency can lead to drug molecules that are too large and liphophilic to make it to market, coining the term ‘molecular obesity‘ to describe the risk that this presents to the fitness of lead compounds. |
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Drugs that go beyond the rule of five – or do they? David S. Millan and colleagues at Pfizer R&D explore the influence of intramolecular hydrogen bonding on the membrane permeability and bioavailability drugs which operate outside of the traditional rule of five – are they actually much closer to rule of five space than previously thought? |
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 New antibiotics to repair faulty genes Jeyakumar Kandasamy et al,. DOI: 10.1039/C0MD00195C Timor Baasov and co-workers developed new aminoglycoside derivatives to suppress nonsense mutations, which result in a variety of genetic diseases, that show enhanced targeting and reduced cell toxicity compared to a leading antibiotic. |
Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship
Shoujun Chen et al., DOI: 10.1039/C0MD00215A
2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization
Ahmed Kamal et al., DOI: 10.1039/C0MD00177E
Impact of ion class and time on oral drug molecular properties
Paul D. Leeson, Stephen A. St-Gallay and Mark C. Wenlock, DOI: 10.1039/C0MD00157K
Structure–activity relationships of methyl-lysine reader antagonists
J. Martin Herold and Stephen V. Frye et al., DOI: 10.1039/C1MD00195G
New insight into the mode of action of vancomycin dimers in bacterial cell wall synthesis
Osamu Yoshida et al., DOI: 10.1039/C0MD00230E
If you would like to continue to receive access to MedChemComm in 2012 please contact sales@rsc.org and ask for a quote.
Additionally, why not consider submitting your next manuscript to the journal? We now also offer optional Accepted Manuscript publication, so that your manuscript is available faster in a citable form.
The first of the International Symposia on Advancing the Chemical Sciences (ISACS) series next year is to be Challenges in Organic Chemistry and Chemical Biology (ISACS7) on 12 – 15 June at the University of Edinburgh, UK.
See the excellent list of confirmed speakers and details of the abstract submission process here.
We are pleased to inform our authors that we will be extending the submission deadline for our forthcoming drug-target residence times web theme issue to Monday 6th February 2012.
The issue will be guest edited by Professor Dr Koen Augustyns (University of Antwerp) and aims collect together in one place some of the latest exciting research from across the breadth of drug residence research.
Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work. In addition, as this is a web-based theme issue, printing of articles will not be held for a specific issue thereby allowing rapid dissemination of the science presented online and in print without delay. Both reviews and primary research are suitable for this issue.
If you would like to contribute to this exciting themed issue, please contact the Editorial Office.
This review from Manfred Jung and colleagues looks at the structural biology and inhibition of bromodomains, enzymatic domains which recognise acetylated lysines residues in modified histones in chromatin. Inhibiting the protein–protein interactions in bromodomains by using small molecules as epigenetic tools is an exciting new area of research, offering potential for new therapeutic approaches.
The review includes:
This hot review is part of our forthcoming themed issue on Epigenetics – keep checking back for more hot research in this theme:
Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy
Silviya D. Furdas, Luca Carlino, Wolfgang Sippl and Manfred Jung
DOI: 10.1039/C1MD00201E
This hot review from Philip Jones, MD Anderson Cancer Center, Texas, examines our understanding of the structure and function of epigenetic enzymes, including lysine and arginine methyltransferases and demethylases, histone acetyl transferases and histone deacetylases, and the chemical probes and tools available to increase our understanding.
It focuses on the development of a second generation of epigenetic agents able to manipulate histone modifications responsible for aberrant epigenetic gene transcription associated with disease states.
Areas covered:
Development of second generation epigenetic agents
Philip Jones
DOI: 10.1039/C1MD00199J
This article is part of our forthcoming themed issue on Epigenetics – check back soon for more hot articles in this issue!
This hot article from Caren Freel Meyers and coworkers describes new inhibitors of DXP synthase, which catalyse an important precursor in the pathogen MEP pathway to isoprenoids. Butylacetylphosphonate was able to selectively inhibit E. coli DXP synthase.
Selective inhibition of E. coli 1-deoxy-D-xylulose-5-phosphate synthase by acetylphosphonates
Jessica M. Smith, Ryan J. Vierling and Caren Freel Meyers
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C1MD00233C
In another step to overcome bacterial resistance to antibiotics, scientists from India have made a new class of triazines. Sixteen compounds showed excellent activity against malaria, say the researchers, preserving the potency of their parent antimalarial drug chloroquine. IC50 values ranged from 1.36 to 4.63ng ml-1.
Synthesis of hybrid 4-anilinoquinoline triazines as potent antimalarial agents, their in silico modeling and bioevaluation as Plasmodium falciparum transketolase and β-hematin inhibitors
Moni Sharma, Kuldeep Chauhan, Shikha S. Chauhan, Ashok Kumar, Shiv Vardan Singh, Jitendra K. Saxena, Pooja Agarwal, Kumkum Srivastava, S. Raja Kumar, Sunil K. Puri, Priyanka Shah, M. I. Siddiqi and Prem M. S. Chauhan
DOI: 10.1039/C1MD00188D
