Roundup of Thursday and Friday #ACSDallas News

Today, we’ve got a double-dose roundup of news stories from the ACS national meeting in Dallas that C&EN published on Thursday, 3/20, and Friday, 3/21: Chemists Convene In Dallas ‘Chemistry & Materials for Energy’ was national conference’s theme Color-Changing Gels Track Food Quality Nano-based materials indicate age, temperature history of perishables Reagent Assembles Ring Motifs Common In Drugs Method builds medium-sized nitrogen heterocycles with challenging substitution patterns Paper Spray Goes Head-To-Head With LC/MS Ambient mass spec method yields comparable results for analysis of tamoxifen in...

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Dallas: A Structural Analysis
Mar20

Dallas: A Structural Analysis

If you haven’t been to an ACS national meeting in Dallas—the last one, if memory serves, was in 1998—there’s a few interesting things to see. This is a summation after spending some time walking the streets here the past week. Located on the Trinity River, Dallas was first settled in the early 1840s when Texas was its own country. A few homesteaders moved into this area and built small log cabins. There’s a reconstructed cabin near the convention center. Dallas is now the ninth largest city in the U.S., with about 1.2 million residents, swollen by an additional 10,000 souls this week with the ACS meeting. Dallas has a compact downtown with a surprising structural diversity when it comes to the architecture of its buildings. The Magnolia Hotel, which dates from 1922, features a neoclassic beaux-arts style common in those days and was once home to Magnolia Petroleum Co., which was one of the forerunners of ExxonMobil. The building is famous for its Pegasus sign placed on the roof. This is the iconic red winged pony you see today on gas pumps. Next door to the Magnolia is the Adolphus Hotel, another beaux-arts building, which opened in 1912. It was built by Adolphus Busch, renowned founder of the Anheuser-Busch company. Another Dallas classic is the original Federal Reserve Bank Building, constructed in 1921, another example of the beaux-arts style. The much larger new Reserve Bank Building is a glass and stone box that is not as easy on the eyes. Yet some of the modern buildings in town have an appreciated distinctive look, such as the polygonal glass Wells Fargo Building. It might at first glance look like a shard of glass, but to the country chemist in the big city it is reminiscent of a crystal of some exotic metal salt. Among the other interesting sights in town, there’s the giant eyeball. This is a 30-foot-tall ocular oddity set up in a park (maybe it is an empty lot) adjacent to the Joule Hotel on Main Street. The big eye got its start as part of a pop culture arts project in Chicago before joining the hotel’s modern art collection. But that still doesn’t explain why someone would create it. I wonder how they moved it here from Chicago? For ACS meeting-goers, another point of interest in Dallas this week has been Pioneer Park, which is adjacent to the convention center. The park features an art installation of a herd of oversized longhorns crossing a stream, pressed on by a pair of cowpokes. Oddly there’s also a cemetery right outside the convention center, where some of Dallas’ founding fathers rest in peace. It was...

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Safety professionals: On the outer fringe or the leading edge?

A guest post by Russ Phifer, a consultant with WC Environmental, executive director of the National Registry of Certified Chemists, and past chair of the ACS Division of Chemical Health & Safety. Cross-posted at The Safety Zone. At the ACS meeting in Dallas this week, it was clear that the safety community continues to try to solidify its place in the chemical enterprise. Although technical programming in our field was a little light for this meeting, there were some excellent presentations. The seemingly routine “Ask Doctor Safety” session held at every meeting suddenly attracted a new audience of young women chemists interested in reproductive health. Neal Langerman of Advanced Chemical Safety and Harry Elston of Midwest Chemical Safety surely gave them a newfound respect for the chemicals they might handle. In the Safety eLearning symposium, Janette de la Rosa Ducut of the University of California, Riverside, and Thor Benzing of the UC Division of Agriculture & Natural Resources opened eyes with an arresting presentation. There were some new faces in the crowd at that session, too. Nevertheless, getting thirty or so people in attendance when other programs are getting hundreds can be a little discouraging. Where exactly do safety professionals and their work fit in the chemistry community? Are we on the fringe or at the leading edge? We don’t make a product. We are permitted to “train,” but generally not to “teach.” We can do research, but it’s far more likely to be data inquiry than in the laboratory. The environmental health and safety field encompasses quite a few CHAS, DCT, CINF, ENVR, SCHB, and CHAL professionals, so it does reach across nearly every other discipline within the chemical enterprise. Our job, every day, is to help keep people safe. But it seems that we still don’t get the respect that we’ve earned. We’re making progress. Every ACS president since at least Ned Heindel has made chemical health and safety at least a small part of their presidential years. Each has contributed a little more to health and safety awareness. Now, Diane Schmidt, the immediate past-chair of the Division of Chemical Health & Safety, is in the first of her three presidential succession years. We know that she has been a tireless worker for chemical safety. Hopefully her term as president will help to further raise the profile of the essential role of safety in the chemical...

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Economist Paula Stephan Talks Chemistry Job Placement at #ACSDallas

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

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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...

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Roundup of Monday #ACSDallas News

Here’s a roundup of news stories from the ACS national meeting in Dallas that C&EN published on Monday, 3/17: Stem Cells Possess Mechanical Memory Growing stem cells in stiff or soft environments influences their future differentiation Role Of Mysterious Folded DNA Structures Revealed At Last Study shows i-motifs and related hairpins activate or repress gene expression I’ll round up Tuesday’s stories tomorrow morning. In the meantime, follow @cenmag and #ACSDallas...

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