Conference Reports
234th American Chemical Society National Meeting
Boston MA 19th-23rd August, 2007.
The picturesque city of Boston offered the perfect setting for the abundance of multidisciplinary research unveiled at the 234th American Chemical Society Annual Meeting; its quaint, almost subdued atmosphere offering an excellent contrast to the excitement of the week. With more than 13,500 scientists in attendance, the Convention and Exhibition Center and over a dozen hotels across the city were overflowing with chemists, all eager to gain and share scientific expertise in their specialist areas. This year’s overall theme was ‘Biotechnology for Health and Wellness’, almost ironically, emphasizing the pharmaceutical industry’s progressive move away from chemicals towards to biotech.
The medicinal chemistry division was just one of 31 technical divisions represented at the conference, and offered up a substantial amount of new chemical data of varied disciplines.
The meeting kicked off with a plethora of preclinical revelations. Curis revealed promising preclinical data and the chemical structure of its small molecule hedgehog agonist CUR 201807, informing the meeting that in a transient focal ischaemic model in rats, it reduced infarct volume and improved neurological deficits. Theravance followed with a presentation on its highlyselective muscarinic acetylcholine receptor 2 antagonist THRX-326151, revealing its chemical structure and positive in vitro and in vivo preclinical results.
Sunday evening saw the first of the poster sessions for the week, offering food, drinks and a bustling environment for enthusiastic chemists to peruse the reports of the chemical expertise of their peers. The hall buzzed with the fast pace of the session, as delegates reviewed the plentiful scientific prospects on show, networking with colleagues and gaining and sharing industry knowledge. Interesting posters included that from Bristol- Myers Squibb, reporting on the structure-activity relationship (SAR) studies that led to the discovery of BMS-711939, a highly-selective PPAR-α agonist derived from muraglitazar, for the treatment of coronary artery disease. It demonstrated excellent in vivo profiles and good pharmacokinetics in preclinical species. Amgen presented a poster detailing the SAR of its vanilloid-1 receptor antagonists for the treatment of pain, revealing the chemical structure of the lead compound. It demonstrated a good pharmacokinetic profile in Sprague Dawley rats and had improved solubility when compared to Amgen’s Phase I compound AMG-517. Other interesting posters included Adolor’s, which detailed the SAR of two chemically-distinct series of iNOS inhibitors, under development for the treatment of neuropathic and inflammatory pain.
Monday evening’s Sci-mix poster session offered a variation to the plentiful parallel symposia of the day in the form of a meet-and-greet furry lobster, which welcomed delegates before they were offered popcorn and beer as an accompaniment to their evening.
Alzheimer’s disease seemed to be the theme later in the week, with Wyeth revealing 2 series of chemically distinct BACE-1 inhibitors, which both demonstrated efficacy in preclinical studies. Johnson & Johnson followed the trend by reporting on the lead in its series of BACE-1 inhibitors. GlaxoSmithKline gave an interesting presentation regarding GSK-4336, the lead in its series of benzoxazepinones, acting as selective androgen receptor modulators for the treatment of androgen deficiency in aging males.
As the week wound down, the schedule remained tight, with Wednesday’s medicinal chemistry being presented in back-to-back parallel oral sessions. Wyeth presented the lead in its series of 5-HT6 antagonists, WAY-101, which has potential in the treatment of depression, anxiety, cognition and feeding disorders. In vivo, it enhanced memory retention in the 48hr delay novel object recognition model in rats, and also blocked the MK-801-induced deficit in the novel object recognition model. Other companies presenting included Cytokine PharmaSciences, which revealed preclinical data for its macrophage migration inhibitory factor inhibitor, CPSI-2705, and Roche, which reported the chemical structure for the lead in its series of GABA-A α5 inverse agonists for Alzheimer’s disease.
Wednesday evening’s extensive, multidisciplinary poster session provided a comprehensive end to a busy day’s schedule, marking the end to the conference’s poster sessions. Among the delegates, who casually enjoyed a glass of wine or a beer, an abundance of new scientific research was once again on display. Of interest, Merck and Amgen presented the chemical structure and preclinical data for their series of bradykinin B1 receptor antagonists, developed as analgesics, and chemokine receptor CXCR3 antagonists, respectively. Additionally, Medarex presented the structure and favourable preclinical results for its cancer treatment MED-2338.
The 2007 Fall ACS once again gave the opportunity for those in the field to showcase the most recent chemical advances in medicinal chemistry, and with over 450 abstract submissions within the division, the expanse of information was not to be taken lightly. As biotechnology continues to dominate in the field of pharmaceuticals, the American Chemical Society remains consistent in highlighting the ongoing importance of medicinal chemistry. Indeed, with the experience and expertise displayed at this conference, the demand for chemical intervention in the field of medicine looks set to continue, with the results offering substantial therapeutic benefits.
The 235th ACS (Spring) meeting will be held in New Orleans, LA, on 6th - 10th April, 2008.
The 235th ACS (Fall) meeting will be held in Philidelphia, PA, on 17th - 21st August, 2008.
Jenna Morris
Pharmaprojects Analyst
