RSC Medicinal Chemistry Blog

Welcome to MedChemComm Issue 4, 2013!

Featuring on this month MedChemComm front cover is the work of Dilip K. Tosh and Kenneth A. Jacobson at the NIH in Bethesda, US:

Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches
Dilip K. Tosh and Kenneth A. Jacobson
DOI: 10.1039/c2md20348k

Free to access for 6 weeks 

This work had recenlty been highlighted on our blogs – why not read the full post here!

Also in this issue, read the review article on Metabolism-guided drug design by Amit S. Kalgutkar et al. at Pfizer Worldwide Research and Development, and much more!

Welcome to this blog taking a look between the covers of this month’s issue of MedChemComm.

This impressive image featuring on the front cover of the issue highlights the work being done by Kyong-Tai Kim and Sung-Kee Chung et al. Kim, Chung et al. have found a blood–brain barrier permeable derivative of trehalose that can prevent the aggregation of polyQ in transfected cells. This derivative was also found to prolong the lifespan and improve motor functions in a transgenic mouse model.

Preparation and evaluation of BBB-permeable trehalose derivatives as potential therapeutic agents for Huntington’s disease
Jungkyun Im, Sangjune Kim, Young-Hun Jeong, Wanil Kim, Dohyun Lee, Woo Sirl Lee, Young-Tae Chang, Kyong-Tai Kim and Sung-Kee Chung
DOI: 10.1039/C2MD20112G

Read the whole article for free for 6 weeks!

Welcome to issue 12 of MedChemComm, the last of 2012. This month we have 10 concise articles and 1 review for you to devour.

On the front cover:

Is this review from our collection on ‘The space in-between small molecules and biologicals’ by James C. Collins and Keith James. Collins and James present a critical analysis of macrocyclization reactions published over the past three years, and based on this propose a ‘macrocyclization efficiency index, Emac,’ which would allow the community to determine the true efficiency of a macrocyclization reaction.

Emac – a comparative index for the assessment of macrocyclization efficiency
James C. Collins and Keith James
DOI: 10.1039/C2MD20176C

On the inside cover:

Is this concise article from Masahiro Goto and colleagues who present their investigations into developing a unique, through the skin, protein-delivery system based on a solid-in-oil nanodispersion that utilizes an oil-based vehicle of proteins.

Transdermal delivery of insulin using a solid-in-oil nanodispersion enhanced by arginine-rich peptides
Yoshiro Tahara, Shota Honda, Noriho Kamiya and Masahiro Goto
DOI: 10.1039/C2MD20059G

Remember both of these articles are free to access for the next 6 weeks!

Get your hands on the last issue of 2012 today.

The interesting image on the front cover of this month’s issue of MedChemComm is courtesy of Neil Vasdev and colleagues. Vasdev et al. present work which is aimed at developing a PET radiotracer based on a hydroxyquinoline chelator, and evaluates its potential for detecting amyloid plaques via imaging studies in transgenic rodent models.

Synthesis and PET imaging studies of [18F]2-fluoroquinolin-8-ol ([18F]CABS13) in transgenic mouse models of Alzheimer’s disease
Neil Vasdev et al.
DOI: 10.1039/C2MD20075A

The inside cover highlights the HOT article of Andreea R. Schmitzer and co-workers who report the factors intrinsic to imidazolium salts that are responsible for the salts’ ionophoric activity, allowing them to act as synthetic ion transporters.

An anion structure–activity relationship of imidazolium-based synthetic transporters
Claude-Rosny Elie, Mathieu Charbonneau and Andreea R. Schmitzer
DOI: 10.1039/C2MD20107K

Download both articles for free for the next 6 weeks.

Also in this issue is this HOT article from James S. Scott:

Reduction of acyl glucuronidation in a series of acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors: the discovery of AZD6925

Issue 9 of MedChemComm has arrived….read it today!

Front cover:

Oral delivery of drugs aims to open up new areas of peptide/protein therapeutics associated with the removal for a need for injections. The major problems facing oral delivery of peptides/proteins is hydrolysis/proteolysis in the gastrointestinal tract and an inefficient uptake mechanism for peptides/proteins from the tract. Robert P. Doyle et al. are interested in the use of the vitamin B12 dietary uptake pathway to address these hurdles. In this paper Doyle et al. report the synthesis, purification and characterisation of a new B₁₂-insulin conjugate attached between the B₁₂ ribose hydroxyl group and insulin PheB1

Examining the effects of vitamin B12 conjugation on the biological activity of insulin: a molecular dynamic and in vivo oral uptake investigation
Susan Clardy-James, Damian G. Allis, Timothy J. Fairchild and Robert P. Doyle

Inside cover:

Doxorubicin (DOX) is a widely adopted chemotherapy treatment for many different varieties of cancer, but its clinical value is limited due to its systemic toxicity. Currently one of the best ways to minimize the dose-related toxic shortcoming of DOX is to encapsulate the drug in various drug-delivery systems. In this paper from Shiqi Peng and co-workers design a novel self-complexation and complexation controlled target drug carrier for DOX delivery.

Self-complexation and complexation-controlled target cancer therapy
Li Li, Ming Zhao, Wenhao Li, Yuji Wang, Zhuge Zhang, Ran An and Shiqi Peng

Also in this issue:

A review from James C. Knight and Frank R. Wuest, from University of Alberta, that aims to provide a comprehensive overview of the application of CXCR4-targeted imaging probes across both nuclear (positron emission tomography/single-photon emission computed tomography) and optical modalities.

Nuclear (PET/SPECT) and optical imaging probes targeting the CXCR4 chemokine receptor

Issue 8 of MedChemComm has arrived and it’s a Natural Products themed issue that is filled to bursting with: nine reviews elegantly summarising the synthesis, biosynthesis, inhibitory properties and targets, and biological functions of natural products, as well as new bioinformatics methods for their identification; and fourteen concise articles describing some of the newest discoveries in the field of natural products.

An example of such a concise article is featured on the inside cover of the issue:

Synthesis and anti-Helicobacter pylori activity of analogues of spirolaxine methyl ether
Ivaylo Dimitrov, Daniel P. Furkert, John D. Fraser, Fiona J. Radcliff, Orla Finch and Margaret A. Brimble
DOI: 10.1039/C2MD00314G

To check out the entire themed issue now click here…

A big thank you must go to the guest editors Professor Christopher Walsh (Harvard University) & Dr Sylvie Garneau-Tsodikova (University of Michigan) for all their hard work, and to all those who have contributed to this issue for making this issue such a success.

Finally, below is a cover suggestion from Amanda J. Hughes et al., which we really liked but which we were unfortunately unable to use on the cover, so we thought we would share it with you here.

Employing a polyketide synthase module and thioesterase in the semipreparative biocatalysis of diverse triketide pyrones
Amanda J. Hughes, Joshua F. Detelich and Adrian T. Keatinge-Clay
DOI: 10.1039/C2MD20013A

The front cover of this issue of MedChemComm highlights the work of Philip J. Johnson, Mikhail Y. Berezin and colleagues. As part of the long term goal of developing nerve specific near infrared (NIR) molecular probes capable of non-invasively assessing peripheral nerve damage, in this concise article Berezin et al. present a study on the identification of a NIR dye suitable for such probes, focusing on a novel highly hydrophilic and functionalisable polymethine dye, and its more hydrophobic analogue indocyanine green.

A NIR dye for development of peripheral nerve targeted probes
Tiffany P. Gustafson,  Ying Yan,  Piyaraj Newton,  Daniel A. Hunter,  Samuel Achilefu,  Walter J. Akers,  Susan E. Mackinnon,  Philip J. Johnson and Mikhail Y. Berezin
DOI: 10.1039/C2MD00297C

Also in this issue is the review by Georges Vauquelin on:
Determination of drug–receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance
DOI: 10.1039/C2MD20015E

View the entire issue here….