The cover of MedChemComm issue 5 is by Rudolf K. Allemann et al., whose concise article presents the synthesis of a series of monohalide mercaptoacrylic acid derivatives, and looks at the structure activity relationship in order to investigate the ability of these molecules to inhibit the Ca2+ activation of calpain-1, which is linked with tissue inflammation.
Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates
Sarah E. Adams, Christian Parr, David J. Miller, Rudolf K. Allemann and Maurice B. Hallett
Med. Chem. Commun., 2012,
As with all our covers, this work will be free to access for the next 6 weeks.
You may also be interested in the 3 reviews in the issue on how enantiomeric pairs reveal that key medicinal chemistry parameters vary more than simple physical property based models can explain, small-molecule inhibitors of dimeric transcription factors and Gd(III) chelates for MRI contrast agents.
Find the entire issue right here