Economist Paula Stephan Talks Chemistry Job Placement at #ACSDallas
Mar19

Economist Paula Stephan Talks Chemistry Job Placement at #ACSDallas

Economist Paula Stephan Talks Chemistry Job Placement at #ACSDallas...

Read More
Liveblogging First-Time Disclosures of Drug Structures from #ACSDallas
Mar19

Liveblogging First-Time Disclosures of Drug Structures from #ACSDallas

Watch this space, chem-keteers. Starting at 2PM Central time TODAY, I’ll be continuing my spring tradition of live-blogging the public unveiling of drug structures from ACS Dallas. This spring’s symposium, unfortunately, only contains one true ‘reveal’ – schizophrenia drug candidate AQW051, from Novartis. The other structures are already public. (Three were covered at prior ACS meetings and are part of a ‘where are they now’ talk). I’ve included vintage hand-drawn structures to refresh our collective memories.   UPDATE 12:00PM Central time- screengrab of the afternoon’s program 1:40PM – grabbed a seat in the second row, by a power outlet. Wifi seems to be behaving. May the liveblogging commence! If you’re on Twitter, watch #ACSMEDI and #ACSDallas hashtags. 2:45PM AQW051 Company: Novartis Institutes for BioMedical Research Meant to treat: cognitive impairment associated with schizophrenia (ie, impairment to memory and decision-making) Mode of action: partial agonist at the alpha7 nicotinic acetylcholine receptor Medicinal chemistry tidbit: Novartis started with a lead called JN403, but cardiotoxicity issues limited progress with this molecule. high throughput screening led to 11 chemical families, including quinuclidine ethers, which led to AQW051. Hurth’s team noticed that changes to the molecule’s phenyl moiety made big differences in selectivity for related receptors and other parameters. Status in the pipeline: Phase II clinical trials Related documents: WO2007068476, WO2007068475, WO2006005608, WO2005123732, WO2004022556; Bioorg. Med. Chem. Lett. 2009, 1287-1291 3:30PM MK-1064 (see above for structure) Company: Merck Research Laboratories Meant to treat: insomnia Mode of action: selective orexin 2 receptor antagonist Medicinal chemistry tidbit: MK-1064 is a more selective version of Merck’s dual-orexin receptor antagonist suvorexant, which after setbacks is on the cusp of reaching the market. Research suggests that orexin 2 plays the primary role in wakefulness, so a more selective antagonist could provide relief from insomnia. Merck’s early orexin 2 receptor antagonists were not sufficiently selective and had metabolic issues (eg, pump proteins). Lowering molecular weight and blocking metabolic hot-spots led to MK-1064 Status in the pipeline: Completed Phase I clinical trials Related documents: ChemMedChem 2014, DOI: 10.1002/cmdc.201300447 ; BMCL 2013, 23, 6620 3:56PM asunaprevir and BMS-791325 (now has generic name – beclabuvir) (structures above) Company: Bristol-Myers Squibb Meant to treat: hepatitis C virus Mode of action: asunaprevir inhibits viral NS3 protease; beclabuvir inhibits viral RNA polymerase, however, it is not a nucleoside mimic and so binds outside the polymerase active site Status in the pipeline: Phase III clinical trials Among several clinical tests discussed in Dallas, asunaprevir and beclabuvir were tested as part of a triple-drug cocktail with daclatasvir, BMS’s experimental NS5A inhibitor. Phase 2b study-The triple regimen dosed for 12 weeks achieved cure rates of up to 94%. Related...

Read More
Guest Post: “Why I Am Blogging on amphoteros.com” by Andrei Yudin
Mar05

Guest Post: “Why I Am Blogging on amphoteros.com” by Andrei Yudin

Today’s guest post is by Andrei Yudin, Professor of Chemistry at the University of Toronto. His research group aims to build new bridges between basic chemistry research and drug discovery. During a sabbatical, Yudin launched a blog, and soon discovered that blogging brings several tangible benefits to his group as well as his research program. You can read his blog at www.amphoteros.com. I have always been intrigued by science blogging, but the barrier to give it a shot of my own has been steep. When I started my sabbatical in July of 2013, I realized that I would have some extra time, making it the best moment for me to begin blogging. The idea of connecting with a target audience of fellow researchers using a new means was especially attractive to me. In addition, as I was running experiments during my sabbatical, my graduate students and faculty colleagues were curious about what it was I was cooking in the lab. I did not want them to think that I was “breaking bad”, so I decided to put it all out there – my successes, my failures, and a good dose of self-ridicule. This is how www.amphoteros.com saw its first post on July 20, 2013. I quickly realized that there were relatively few research-oriented chemistry blogs, which stands in contrast to other disciplines such as biology. While the culture of chemistry is different and chemists do not often feel the need to collaborate with one another, our craft is becoming more interdisciplinary and new ways of communicating scientific findings and/or sharing opinions are only going to help. At the moment, amphoteros is driven by my keen interest in science advances both basic and applied. People ask me how I find time for writing and coming up with original subject matter on a daily basis. I somehow do not feel challenged by this: there is always something “bloggable” I can come up with during my train ride back home. I cover a range of subjects and I always look forward to the feedback I get from the readers. The usual way I conceive my posts is by thinking about one of the dominant thoughts that has been consuming me on a given day. Typically, these musings are related to a particular publication, although I do not make a distinction between what’s current and what’s old. To me, something that is important, yet published 50 years ago, is current. In terms of content, I like to have a lot of graphics on my posts. This gives me a chance to practice ideas for my future lecture presentations. In academia, we always think...

Read More
This Week on CENtral Science: #FlameChallenge 3, Informex, and more
Jan31

This Week on CENtral Science: #FlameChallenge 3, Informex, and more

Tweet (with Instagram!!) of the Week: When chemists get cooking #realtimechem #AlchemusRocks http://t.co/18TZhZCe8u — Laura Jane (@laurajane0103) January 31, 2014 To the Network: Fine Line: State of the Vibe Just Another Electron Pusher: I’ll get around to procrastinating later Newscripts: Flame Challenge 2014 and Amusing News Aliquots Terra Sigillata: Promoting Chemistry’s Positive Public Image The Watch Glass: All-Chemical All-American Football Team and Equipment Mart and Thermoelectric Materials and...

Read More
This Week on CENtral Science: Informex #inf14 , Industrial Accidents, and More
Jan24

This Week on CENtral Science: Informex #inf14 , Industrial Accidents, and More

Apparently, Gmail was down today. (Sarcasm there. I certainly noticed.) Plenty of Gmail tweets out there, but this wins: Tweet of the Week: So I discovered something about the #LEGO #Scientist – she is a fellow fluorescence researcher! #realtimechem pic.twitter.com/WnCwtaf7og — Brian Wagner (@DrummerBoy2112) January 24, 2014 To the Network: Fine Line: C&EN Talks at Informex and Buh-buh-buh-buh-buh-Bad! and Ohhhhhhhhh~ Miami! Newscripts: Amusing News Aliquots The Safety Zone: Prosecuting companies rather than executives for wrongdoing The Watch Glass: High Temperature Superconductors and Supercritical...

Read More