Some news from London

Over the past several days I have been in London, England, where I attended the Fall Board Meeting of Organic and Biomolecular Chemistry. Richard Kelly, the Managing Editor of this RSC publication, has put this meeting together in the Mayfair district of London. Jeff Bode (ETH, Zurich) is stepping down as the Board Chairman and I will be taking over his responsibilities from January 2015. I have to tip my hat off to Jeff for his leadership over the past several years. I have thoroughly enjoyed my role of one of the Associate Editors. The difference now will be that I am no longer going to handle manuscripts, but will instead oversee some strategic areas for growth and improvement. I think this will be very exciting. Earlier this week, I had a lot of fun together with Jeff as well as Ashraf Brik of Ben Gurion University, Margaret Brimble of the University of Aukland, Tony Davis of the University of Bristol, Jonathan Clayden of the University of Manchester, Pauline Chiu of the University of Hong Kong, and Paolo Scrimin of the University of Padova. Unfortunately, Jin-Quan Yu of Scripps was not able to make it to this meeting. Along with Margaret and I, Jin-Quan is one of OBC’s Associate Editors.

In terms of chemistry, I actually wanted to share something that relates to the work of Margaret Brimble (she flew in all the way from New Zealand to meet us). Margaret brought along some exciting news: NNZ-2566, a molecule developed as part of a collaboration between her lab and Neuren Pharma, was recently approved by the FDA, which has granted orphan drug designation to NNZ-2566 for treatment of Fragile X Syndrome. This tripeptide also demonstrates neuroprotective efficacy in models of traumatic brain injury such as concussion. Evidently, the U.S. Army is very interested in NNZ-2566, although not much is known about the mechanism of action of this exciting compound. What I found remarkable is that the tripeptide is orally bioavailable. The C-methyl proline residue makes this molecule considerably more stable than the corresponding non-methylated congener. The methyl group really “messes up” with the nearby amide bond, which apparently drives the logD down and improves the pharmacological profile of NNZ-2566. I have always thought that there is something special about C-methylproline…

uy

http://www.neurenpharma.com/irm/content/nnz-2566-in-rett-syndrome.aspx?RID=330

4 thoughts on “Some news from London

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