Lorena Tomas Laudo – RSC Medicinal Chemistry Blog

Author Archive

HOT: Imaging Alzheimer’s disease brains

04 May 2011

Senile plaques (SPs) and neurofibrillary tangles (NFTs) are two pathological hallmarks for Alzheimer’s disease. Unfortunately, there is no an effective and simple diagnostic method to detect them.

In this paper, Masahiro Ono, Hideo Saji and colleagues at Kyoto University, have developed a series of radioiodinated phenyldiazenyl benzothiazole (PBD) derivatives as probes for the imaging of NFTs in the brain. Imaging agents need to be able to both penetrate the blood-brain barrier after an intravenous injections and be rapidly washed out from the normal brain. Unfortunately, even though these radioiodinated PDB derivatives displayed high affinity for tau aggregates and good brain uptake, the persistent radioactivity in the brain made them unsuitable for imaging NFTs in vivo.

If you want to find out more about these ‘inspiring’ imaging agents, you can download the article for free.

Phenyldiazenyl benzothiazole derivatives as probes for in vivo imaging of neurofibrillary tangles in Alzheimer’s disease brains
Kenji Matsumura, Masahiro Ono, Shun Hayashi, Hiroyuki Kimura, Yoko Okamoto, Masafumi Ihara, Ryosuke Takahashi, Hiroshi Mori and Hideo Saji
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00034A

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MedChemComm delighted to meet authors!

18 Apr 2011

The Royal Society of Chemistry was present in Anaheim for the ACS Spring 2011 National Meeting and Exposition last March. Very hectic few days full of Journal celebrations, product demos and workshops.

We were very happy to hear that one of our MedChemComm authors, Jose Medina Franco, paid the RSC booth a visit.
Here you can see him with a copy of MedChemComm Issue 1, where his article was published.

Thanks to Jose for dropping by! You can now read his article, which is free to access here.

Structure–activity relationships of benzimidazole derivatives as antiparasitic agents: Dual activity-difference (DAD) maps
Jaime Pérez-Villanueva, Radleigh Santos, Alicia Hernández-Campos, Marc A. Giulianotti, Rafael Castillo and Jose L. Medina-Franco
Med. Chem. Commun., 2011, 2, 44-49
DOI: 10.1039/C0MD00159G

If you want to find out where we are going this year and you want to come and meet us, like Jose did, we would love to hear from you. These are the list of conferences we are planning to go to:

Lakeland Heterocyclic meeting, May – Grasmere, UK
ACS National Organic Symposium – 5th – 9th June – Princeton, US
Frontiers in Medicinal Chemistry Meeting: Emerging Targets, Novel Candidates and Innovative Strategies- 19th-21st July – Stockholm, Sweden
International Symposium on Macrocyclic and Supramolecular Chemistry (ISMSC) – 3rd-7th July, Brighton, UK
European Symposium on Organic Chemistry – 10th-15th July, Crete, Greece
22nd International Symposium: Synthesis in Organic Chemistry – 11th-14th July, Cambridge, UK
OMCOS 16 – 24th-28th July – Shanghai, China
GRC Medicinal Chemistry – 7th – 12th August – New Hampshire, US
4th International Symposium on Advances in Synthetic and Medicinal Chemistry – 21st-25th August, St Petersburg, Russia
242nd Meeting of the American Chemical Society- 27th – 31st August, Denver, US
16th RSC-SCI Medicinal Chemistry meeting – 11th-14th September, Cambridge, UK

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Molecular obesity is weighing down drug discovery-MedChemComm in Chemistry World

07 Apr 2011

As we anticipated, Michael Hann’s review on molecular obesity has attracted loads of interest.

Chemistry World publishes a comment on this paper in the April Issue.

You can read the full story here and download the paper which is free to access here.

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00017A

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MedChemComm Issue 3 is here

10 Mar 2011

Welcome to MedChemComm Issue 3!

In this new issue, you’ll find a new collection of exciting papers on medicinal chemistry research, which you can download for free!

This month’s menu includes:

– The importance of solvation in the design of ligands targeting membrane proteins

– Repairing faulty genes by aminoglycosides: Identification of new pharmacophore with enhanced suppression of disease-causing nonsense mutations

– Synthesis and anti HSV-1 evaluation of novel indole-3,4-diones

– Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship

– Scaffold-hopping from aminoglycosides to small synthetic inhibitors of bacterial protein biosynthesis using a pseudoreceptor model

– The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection

– Synthesis and biological evaluation of novel ferrocenyl curcuminoid derivatives

– Interactions of polysulfanes with components of red blood cells

– Structure-based design, synthesis, and profiling of potent and selective neuronal nitric oxide synthase (nNOS) inhibitors with an amidinothiophene hydroxypiperidine scaffold

– Carba-LNA modified siRNAs targeting HIV-1 TAR region downregulate HIV-1 replication successfully with enhanced potency

That is a great selection, isn’t it? We hope you enjoy it and you find it enlightening.

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MedChemComm in The Korea Herald

22 Feb 2011

MedChemComm article by Chung Sung-kee and co-workers has been highlighted in The Korea Herald.

A group of South Korean researchers said Monday that they found a way to use drugs to fight brain tumors that are currently treated with only surgery and chemotherapy.

You can read the whole story here and also download the article which is free to access here.

Preparation of blood-brain barrier-permeable paclitaxel-carrier conjugate and its chemotherapeutic activity in the mouse glioblastoma model
Juyoun Jin, Woo Sirl Lee, Kyeung Min Joo, Kaustabh K. Maiti, Goutam Biswas, Wanil Kim, Kyong-Tai Kim, Se Jeong Lee, Kang-Ho Kim, Do-Hyun Nam and Sung-Kee Chung
Med. Chem. Commun., 2011
DOI: 10.1039/C0MD00235F

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Repairing faulty genes – Baasov and MedChemComm in Chemistry World

22 Feb 2011

Israeli scientists have developed compounds that could be better treatments for genetic diseases than current drugs.

Timor Baasov and his colleagues at the Israel Institute of Technology have improved compounds used to suppress faults in genes called nonsense mutations.

‘Treating genetic disorders is one of the biggest challenges of modern medicine. The likelihood that suppression therapy could be used clinically is very feasible,’ says Baasov.

Read the whole story in Chemistry World.

The full paper is free to access here:

Repairing faulty genes by aminoglycosides: Identification of new pharmacophore with enhanced suppression of disease-causing nonsense mutations
Jeyakumar Kandasamy, Dana Atia-Glikin, Valery Belakhov and Timor Baasov,
Med. Chem. Commun., 2011
DOI: 10.1039/c0md00195c

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Fighting back against antibiotic resistant bacteria-MedChemComm in Chemistry World

11 Feb 2011

Scientists in Japan have revealed how vancomycin dimers are effective against vancomycin-resistant bacteria.

Vancomycin, a glycopeptide antibiotic, is used to treat bacterial infections in cases when other antibiotics are ineffective. However, the development of vancomycin resistant enterococci (VRE) and Staphylococcus aureus means that researchers are turning to different forms of vancomycin to improve its efficacy.

Hirokazu Arimoto at Tohoku University, Sendai, and colleagues had previously shown that vancomycin dimers displayed excellent antibacterial activity against vancomycin-resistant bacteria. Now, they have shown how the dimers interact with the bacteria.

Read the full story in Chemistry World.

The paper is free to access!

New insight into the mode of action of vancomycin dimers in bacterial cell wall synthesis
Osamu Yoshida, Jun Nakamura, Hidenori Yamashiro, Kenji Miura, Sayaka Hayashi, Kosei Umetsu, Shu Xu, Hideki Maki and Hirokazu Arimoto
Med. Chem. Commun., 2011
DOI: 10.1039/c0md00230e

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MedChemComm Issue 2 published on line- Free access!

11 Feb 2011

Our second issue of MedChemComm 2011 is here already!

This new and exciting issue comes with two reviews.
The first one by Paul Leeson and collegues on the impact of ion class and the time on the properties of oral drugs and the second one by Peter Kovacic and Ratnasamy Somanathan on the mechanisms of aromatic primary amines and the influence on the physiological activity.

The issue also contains six vibrant concise articles that bring you the best medicinal chemistry research.
From 2D and 3D activity landscape representations to imaging contrast agents. For those of you who are more synthetic medchems you can find articles on the synthesis and biological activities of AA-Trp-Trp-OBzl and isoquinolones. We close the issue with a study of activation energies and their influence in the stability of drugs and a final article on HIV-integrase inhibitors.

What do you think? We would like to receive your feedback on the new RSC medicinal chemistry journal MedChemComm!

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Combating cold sores – MedChemComm in Chemistry World

01 Feb 2011

This MedChemComm article by Giovanni Grassi and colleagues in Messina, Italy, has been highlighted in the RSC magazine Chemistry World.

New compounds to fight the herpes simplex virus (HSV-1), which causes cold sores, have been made by researchers from Italy. The compounds’ antiviral activity could be enhanced further by encapsulating them in a cyclodextrin nanocarrier that acts as a delivery system.

Giovanni Grassi and colleagues from the University of Messina made indole-3,4-diones that share structural features with inhibitors of kinase – an enzyme linked to many diseases. The inhibitors were recently reported to prevent viral replication in vitro. ‘The diones showed remarkable anti HSV-1 activity in vitro,’ says Grassi. They then encapsulated the most effective dione in an amphiphilic – both hydrophilic and lipophilic – cyclodextrin. These nanocarriers increased the ability of the antiviral agents to penetrate into target cells.

Read the full story here.

The article is now free to access and you can download it here.

Synthesis and anti HSV-1 evaluation of novel indole-3,4-diones
Angela Scala, Massimiliano Cordaro, Antonino Mazzaglia, Francesco Risitano, Assunta Venuti, Maria Teresa Sciortino and Giovanni Grassi, Med. Chem. Commun., 2011
DOI: 10.1039/c0md00190b

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MedChemComm Issue 1 2011 is now published!

12 Jan 2011

Welcome to MedChemComm Issue 1 of the New Year!

2011 is going to be a very exciting year for MedChemComm and you will still be able to read all our content for free until the end of the year. You just need to register for a RSC personal account.
We also encourage you to keep up-to-date with the latest news by following us on Twitter, signing up for our e-alerts and receiving MedChemComments (our newsletter) in your inbox.

Don’t forget to keep an eye on the MedChemComm Blog! You can also sign up for our RSS feed.

Without further delay, here you have the first issue of 2011.

We start the year with a great selection of articles, including ‘Proteochemometric Modeling as a Tool to Design Selective Compounds and Extrapolating to Novel Targets’ by Andreas Bender et al. and ‘Evaluation of FR901464 analogues in vitro and in vivo’ by Kazunori Koide et al.

I hope you find the articles interesting and you consider submitting your research to MedChemComm in the near future.

From the MedChemComm editorial office we wanted to wish a very happy New Year to all our readers, authors and referees and a very successful one in medicinal chemistry.

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RSC Medicinal Chemistry Blog