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Q2 top 10 for MedChemComm

13 Aug 2013

Please take a look at the top 10 most accessed MedChemComm articles for the second quarter of 2013:

Metabolism-guided drug design
Antonia F. Stepan, Vincent Mascitti, Kevin Beaumont and Amit S. Kalgutkar
Med. Chem. Commun., 2013, 4, 631-652
DOI: 10.1039/C2MD20317K

Synthesis and antiproliferative activity of some 3-(pyrid-2-yl)-pyrazolines
Alexander Ciupa, Paul A. De Bank, Mary F. Mahon, Pauline J. Wood and Lorenzo Caggiano
Med. Chem. Commun., 2013, 4, 956-961
DOI: 10.1039/C3MD00077J

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011, 2, 1135-1161
DOI: 10.1039/C1MD00134E

A critical assessment of modeling safety-related drug attrition
Daniel Muthas, Scott Boyer and Catrin Hasselgren
Med. Chem. Commun., 2013, 4, 1058-1065
DOI: 10.1039/C3MD00072A

Increasing small molecule drug developability in sub-optimal chemical space
Timothy J. Ritchie, Simon J. F. Macdonald, Simon Peace, Stephen D. Pickett and Christopher N. Luscombe
Med. Chem. Commun., 2013, 4, 673-680
DOI: 10.1039/C3MD00003F

Recent applications of multicomponent reactions in medicinal chemistry
Paul Slobbe, Eelco Ruijter and Romano V. A. Orru
Med. Chem. Commun., 2012, 3, 1189-1218
DOI: 10.1039/C2MD20089A

On the origins of drug polypharmacology
Xavier Jalencas and Jordi Mestres
Med. Chem. Commun., 2013, 4, 80-87
DOI: 10.1039/C2MD20242E

Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications
Paul C. Trippier and Christopher McGuigan
Med. Chem. Commun., 2010, 1, 183-198
DOI: 10.1039/C0MD00119H

Silver nanoparticles—the real “silver bullet” in clinical medicine?
Kenneth K. Y. Wong and Xuelai Liu
Med. Chem. Commun., 2010, 1, 125-131
DOI: 10.1039/C0MD00069H

The use of phosphate bioisosteres in medicinal chemistry and chemical biology
Thomas S. Elliott, Aine Slowey, Yulin Ye and Stuart J. Conway
Med. Chem. Commun., 2012, 3, 735-751
DOI: 10.1039/C2MD20079A

We very much welcome your thoughts and comments below:

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MedChemComm Top 10 most accessed articles published in 2012 (Volume 3)

15 Apr 2013

Curious about which articles published in 2012 gathered most readership? Here are the Top 10 works your colleagues have been accessing most in MedChemComm:

The developability of heteroaromatic and heteroaliphatic rings – do some have a better pedigree as potential drug molecules than others?
Timothy J. Ritchie, Simon J. F. Macdonald, Simon Peace, Stephen D. Pickett and Christopher N. Luscombe
Med. Chem. Commun., 2012, 3, 1062-1069
DOI: 10.1039/C2MD20111A

Gd(III) chelates for MRI contrast agents: from high relaxivity to “smart”, from blood pool to blood–brain barrier permeable
Chang-Tong Yang and Kai-Hsiang Chuang
Med. Chem. Commun., 2012, 3, 552-565
DOI: 10.1039/C2MD00279E

Development of second generation epigenetic agents
Philip Jones
Med. Chem. Commun., 2012, 3, 135-161
DOI: 10.1039/C1MD00199J

Small molecules DNA methyltransferases inhibitors
Nadine Martinet, Benoît Y. Michel, Philippe Bertrand and Rachid Benhida
Med. Chem. Commun., 2012, 3, 263-273
DOI: 10.1039/C1MD00194A

Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy
Silviya D. Furdas, Luca Carlino, Wolfgang Sippl and Manfred Jung
Med. Chem. Commun., 2012, 3, 123-134
DOI: 10.1039/C1MD00201E

Epigenetics—an emerging and highly promising source of new drug targets
Nessa Carey
Med. Chem. Commun., 2012, 3, 162-166
DOI: 10.1039/C1MD00264C

From the protein’s perspective: the benefits and challenges of protein structure-based pharmacophore modeling
Marijn P. A. Sanders, Ross McGuire, Luc Roumen, Iwan J. P. de Esch, Jacob de Vlieg, Jan P. G. Klomp and Chris de Graaf
Med. Chem. Commun., 2012, 3, 28-38
DOI: 10.1039/C1MD00210D

Inhibitors of Stat5 protein signalling
Abbarna A. Cumaraswamy, Aleksandra Todic, Diana Resetca, Mark D. Minden and Patrick T. Gunning
Med. Chem. Commun., 2012, 3, 22-27
DOI: 10.1039/C1MD00175B

Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target
Duncan C. Miller, Graham Lunn, Peter Jones, Yogesh Sabnis, Nichola L. Davies and Paul Driscoll
Med. Chem. Commun., 2012, 3, 449-452
DOI: 10.1039/C2MD00270A

Interested in submitting your own work to MedChemComm? Submit online today, or email us with your suggestions!

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Chemical biology and medicinal: Ionic liquids could aid in the delivery of active pharmaceutical compounds in the body

12 Feb 2013

US scientists have provided a strategy to improve the properties of active pharmaceutical ingredients (APIs) by combining ionic liquids (used to improve the properties of solid APIs) with prodrugs (used to improve solubility, permeability and bioavailability of APIs). The prodrug ionic liquids present additional advantages such as controlled release of the APIs in simulated body fluids. This work could offer an important strategy to improve the properties of APIs and drug delivery.

Prodrug ionic liquids: functionalizing neutral active pharmaceutical ingredients to take advantage of the ionic liquid form
O. Andreea Cojocaru, Katharina Bica, Gabriela Gurau, Asako Narita, Parker D. McCrary, Julia L. Shamshina, Patrick S. Barber and Robin D. Rogers
MedChemComm, 2013
DOI: 10.1039/C3MD20359J

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Chemical biology and medicinal: Modulation of ghrelin signalling for the treatment of obesity

22 Jan 2013

Scientists in the UK and Sweden have identified compounds that work against a ligand (ghrelin) that’s part of a growth hormone that’s thought to increase the amount of food we eat. The compounds could be used to prevent obesity and diabetes.

Ghrelin, a 28 amino acid acylated peptide hormone, is the endogenous ligand of growth hormone secretagogue receptor type 1a (GHS-R1a), and is thought to control food intake. Acylated ghrelin is released from mucosal cells in response to hunger cues, resulting in a peak of plasma ghrelin levels before meals. It has also been shown that ghrelin infusion in both rodents and humans increases appetite and food intake. Therefore, peripheral and central nervous system (CNS) penetrant ghrelin receptor antagonists could be a potential cure for obesity and diabetes.

In this work, the team identified a tool compound within a pyrazolo-pyrimidinone based series of GHS-R1a antagonists that had good overall properties and sufficient oral plasma and CNS exposure to demonstrate reduced food intake in mice through a mechanism involving GHS-R1a.

Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity
William McCoull, Peter Barton, Anders Broo, Alastair Brown, David Clarke, Gareth Coope, Rob D M Davies, Alastair Dossetter, Elizabeth Kelly, Laurent Knerr, Philip Macfaul, Jane Holmes, Nathaniel Martin, Jane E Moore, David Morgan, Claire Newton, Krister Osterlund, Graeme Robb, Eleanor Rosevere, Nidhal Selmi, Stephen Stokes, Tor Svensson, Victoria Ullah and Emma Williams
Med. Chem. Commun.
DOI: 10.1039/C2MD20340E

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MedChemComm Emerging Investigator Lectureship award – nominations now open!

26 Nov 2012

Voting for the MedChemComm Emerging Investigator Lectureship is now open. This annual Lectureship recognises an emerging scientist who has made a significant contribution to medicinal chemistry or a related field in the early part of their independent career.

To make a nomination, please contact the MedChemComm Editorial Office with both the name and affiliation of the person you are nominating along with a brief description of why they should be considered. All members of the community are eligible to vote; however, nominated individuals must have published their work in MedChemComm in order to be eligible for entry. Nominees must also have completed their PhD on or after the 31st December 2002.

Closing date for Nominations is the 31^st December 2012

The decision to award the Lectureship will be made by a panel of MedChemComm Editorial Board members. The receipient will receive a contribution towards speaking at a conference of their choice.

This year’s winner Dr Patrick Gunning, (University of Toronto, Canada) was presented with the Lectureship due to his prominent work into the investigation and manipulation of protein function. He will be presenting a lecture at an international conference in 2013.

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Chemical biology and medicinal: Optimising compounds for diabetes treatment

12 Nov 2012

Scientists have optimised a series of compounds that have the potential to treat diabetes and obesity.
The drug candidates work by inhibiting the enzyme diacylglycerol acetyl transferase 1, which is responsible for catalysing the production of triglycerides. Excessive levels of triglycerides contribute to metabolic syndrome, which increases risk of diabetes, heart disease and stroke. Previous drug inhibitors have been unsuccessful in clinical trials due to low solubility. The optimised compounds are highly soluble and exhibit excellent potency for their target.

Graphical Abstract

Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353
Michael J. Waring, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Leonie Campbell, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Philip A. MacFaul, Charles O’Donnell and Andrew V. Turnbull
Med. Chem. Commun., DOI: 10.1039/C2MD20190A

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RSC Medicinal Chemistry Blog

Author Archive

Q2 top 10 for MedChemComm

MedChemComm Top 10 most accessed articles published in 2012 (Volume 3)

Chemical biology and medicinal: Ionic liquids could aid in the delivery of active pharmaceutical compounds in the body

Chemical biology and medicinal: Modulation of ghrelin signalling for the treatment of obesity

MedChemComm Emerging Investigator Lectureship award – nominations now open!

Chemical biology and medicinal: Optimising compounds for diabetes treatment

Top ten most accessed articles in July 2012

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