Heterocyclic Chemistry: Synthesis, Chemical Biology, and Drug Discovery

Conveners: 

Keith Jones, Institute of Cancer Research, UK

Colin Suckling, University of Strathclyde, Glasgow, UK

Programme:

Monday 3 August (morning and afternoon)

Tuesday 4 August (morning and afternoon)

Keynote Speakers

Cyclization, catenation and PCR amplification of DNA ligated by click chemistry
Tom Brown, University of Southampton, UK

Nitrogen heterocycles a versatile class for antiparasitic chemotherapy
P.M.S. Chauhan, Central Drug Research Institute, Lucknow, India

Protein epitope mimetics in drug and vaccine research
John A. Robinson, University of Zurich, Switzerland

Defining the druggable cysteinome
Jack Taunton, University of California, San Francisco, USA

Speakers

An improved direct synthetic approach to anhydronucleosides
Nouria A. Al-awadi, Kuwait University, Kuwait

Hydrogen bonding and hydrophobic interactions in highly potent antibacterial minor groove binders
David Breen, University of Strathclyde, UK

Development of potent inhibitors of the DNA-dependent protein kinase (DNA-PK)
Celine Cano, Newcastle University, UK

Discovery of SCH 530348 - A thrombin receptor antagonist (TRA) with potent antiplatelet activity
Samuel Chackalamannil, Schering-Plough Research Institute, USA

Stereoselective Synthesis of Aza CMI-977, a potential lead candidate for chronic asthma
Mukund Chorghade, Chorghade Enterprises / THINQ Pharma, USA

Recent progress in the total synthesis of gambieric acid A, a marine polyether with potent anti-fungal activity
J. Stephen Clark, University of Glasgow, UK

Enantioselective synthesis of beta-carboline and isoquinoline derivatives via the asymmetric transfer hydrogenation
Zbigniew Czarnocki, University of Warsaw, Poland

Novel benzimidazole-pyrimidine conjugates as potent antiviral agents
Hoda I. El Diwani, National Research Centre, Cairo, Egypt

Asymmetric synthesis of highly substituted piperidines as kappa opioid receptor antagonists
Stephen M. Husbands, University of Bath, UK

Novel pyrazoline and pyrazole amino acids by 1,3-dipolar cycloaddition
Raymond C.F. Jones, Loughborough University, UK

The discovery of Sugammadex (Bridion®)
Ronald Palin, Schering-Plough, UK

Synthesis of novel 2-pyrazolines
Geeta J. Pant, H.N.B. Garhwal University, India

Towards the total synthesis of the ajmaline family of indole alkaloids
Tess Philips, Keele University, UK

The stereoselective synthesis of iodinated analogues of reboxetine for SPECT imaging of the noradrenaline transporter
Andrew Sutherland, University of Glasgow, UK

PK/PD optimization of dihydropyridine allosteric FSH-receptor agonists
Cornelis M. Timmers, Schering-Plough Research Institute, The Netherlands

Title TBA
Nicholas J. Westwood, University of St Andrews, UK

Symposium Information

More than 90% of new drugs contain heterocycles and the interface between chemistry and biology, at which so much new scientific insight, discovery, and application is taking place is crossed by heterocyclic compounds.

The essential science upon which these advances are based is the synthesis of designed heterocyclic compounds which make it possible to probe sensitively the key events in biology in partnership with structural biology.

To organise the vast amount of new information becoming available, chemical informatics plays a key role. All of these sciences feed into the creation of opportunities for the discovery of new effective and successful drugs.