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Chairpersons Anna Maria Papini, University of Florence (Italy) György Dormán, ComGenex Inc., Budapest (Hungary) Scientific Committee Mark Bradley, University of Southampton (United Kingdom) Alberto Brandi, University of Florence (Italy) György Dormán, ComGenex Inc., Budapest (Hungary) Ferenc Darvas, ComGenex Inc., Budapest (Hungary) C. Oliver Kappe, University of Graz (Austria) Anna Maria Papini, University of Florence (Italy) Antonello Pessi, IRBM, Merck Rome, Pomezia (Italy) Paolo Rovero, University of Salerno (Italy) Andrea Basso, University of Genoa (Italy) Secretariat Beatrix Molnár, ComGenex Inc., Budapest (Hungary), E-mail: [email protected] Martina Vestrucci and Chiara Tagliavini, Ufficio di Coordinamento, Polo Scientifico, University of Florence (Italy), E-mail: [email protected] Innovative Combinatorial Approaches and Technologies 1st Practical Training Course Polo Scientifico, University of Florence Italy April 9-11, 2003 Staff Maria Claudia Alcaro, Pietro Campiglia, Marco Cecchi, Martina Gensini, Katalin Szommer Kocsis, András Lukács, Barbara Mulinacci, Francesca Nuti, Elisa Peroni, Giuseppina Sabatino, Maria Salvati Organization Giovanni Pisaturo, Ufficio di Coordinamento, Polo Scientifico, University of Florence (Italy) Sponsors Advanced ChemTech, Argonaut, Büchi, CEM, Comgenex Inc., CSF, FKV, Genevac, Merck Biosciences, Milestone, Mimotopes, Novabiochem, Personal Chemistry, Radley, Sigma-Aldrich, Stepbio, ThermoFinnigan, UnionBiometrica, Zinsser. Chemicals for practical sessions are kindly provided by MerckBiosciences, Novabiochem and Sigma-Aldrich http://www.combichem.org/florencecourse.htm Wednesday, April 9TH 2003 Aula Magna, Polo Scientifico, Via Bernardini 6, Sesto Fiorentino (FI) 8:30-9:00 Opening remarks: “Benvenuti a Firenze” Address from ESCS, Dr. Ferenc Darvas DESIGN Theoretical Design 9.00-10.00 Derek Reynolds, REYTEK Limited, Bedford (United Kingdom) «Fragment Based Library Design» 10.00–11.00 Hugo Kubinyi, Weisenheim am Sand (Germany) «Combinatorial Library Design (Virtual Screening)» 11.00-11.30 Coffee break, Exhibits (room 57, 1st floor) Applied Design 11.30-12.30 Dimitris K. Agrafiotis, 3-Dimensional Pharmaceuticals, Exton (USA) «Novel computational tools for library analysis» SYNTHESIS & CHARACTERIZATION 12.30-13.30 György Dormán, ComGenex Inc., Budapest (Hungary) «Combinatorial Approaches in Chemical Genomics» 13.30–14.30 Lunch, Exhibits (room 57, 1st floor) 14.30-15.30 Menotti Ruvo, Istituto di Biostrutture e Bioimmagini, Naples (Italy) «Synthesis and screening of peptide libraries» 15.30-16.30 Antonio Guarna, University of Florence (Italy) «Solution and solid phase synthesis of peptidomimetic libraries» PRACTICAL SESSION Lab. 286, Polo Scientifico, Via della Lastruccia 3, Sesto Fiorentino (FI) 17.00-19.00 INSTRUMENTS FOR PARALLEL SYNTHESIS Experiences of 30 minutes each, participants will be divided in groups Stefano Giovanninetti, Stepbio-Radley «Parallel synthesis and work-up of aromatic ketons: evaluation of different catalytic systems» György Dormán, ComGenex Inc., Budapest (Hungary) «ComGenex Parallel Synthesizer» Annick Vancolen, Advanced ChemTech «LabMate, PLS 4X4, APEX 396, ACTEvap» Gerhard Schonenberger and Simone Giordano, Büchi «Syncore Semi-automated Solution and Solid Phase Parallel Synthesizer» Thursday, April 10TH 2003 Aula Magna, Polo Scientifico, Via Bernardini 6, Sesto Fiorentino (FI) SYNTHESIS & CHARACTERIZATION Advanced Solid-Phase Techniques 9.00-10.00 Mark Bradley, University of Southampton (United Kingdom) «Support and innovative handling methods for solid phase synthesis» 10.00–11.00 Andrea Basso, University of Genoa (Italy) «Multicomponent reactions in solid-phase organic synthesis» 11.00-11.30 Coffee break, Exhibits (room 57, 1st floor) PRACTICAL SESSION Lab. 286, Polo Scientifico, Via della Lastruccia 3, Sesto Fiorentino (FI) 14.30-17.00 Menotti Ruvo, Istituto di Biostrutture e Bioimmagini, Naples (Italy) «Split&Mix approach to a 3x3 peptide library synthesis» 17.00-17.45 Simone Giordano, Büchi «Parallel filtration post solid-phase synthesis» Aula 186, Polo Scientifico, Via della Lastruccia 3, Sesto Fiorentino (FI) 17.45-18.15 Andrea Basso, University of Genoa (Italy) «Mimotopes Lanterns» 18.15-18.45 Werner Zinsser, Zinsser Analytic «New tool for automated parallel synthesis» Solution Phase Parallel Synthesis 11.30-12.30 Ferenc Darvas, ComGenex Inc., Budapest (Hungary) «Solution-phase parallel synthesis platforms. HT liquid-liquid extraction and purification platforms » 18.45-19.00 Maria Claudia Alcaro, ThermoFinnigan «ESI-MS characterization of the result of the synthesis performed during the practical sessions» Analysis 12.30-13.30 Tamás Karancsi, ComGenex Inc., Budapest (Hungary) «HT analytical approaches » 13.30–14.30 Lunch, Exhibits (room 57, 1st floor) SOCIAL EVENTS Villa Agape Via Torre del Gallo n. 8, Firenze 20.30 Social Dinner Friday, April 11TH 2003 Aula Magna, Polo Scientifico, Via Bernardini 6, Sesto Fiorentino (FI) COMBINATORIAL APPROACHES PRACTICAL SESSION Lab. 286, Polo Scientifico, Via della Lastruccia 3, Sesto Fiorentino (FI) 14.30-16.00 MICROWAVE-ASSISTED COMBINATORIAL CHEMISTRY Experiences of 30 minutes each, participants will be divided in groups Advanced techniques Tony Lewis and Wolfgang Vogel, Personal Chemistry «Microwave assisted Hantzsch synthesis» 9.00-10.00 Oliver Kappe, University of Graz (Austria) «Microwave–Assisted Organic and Combinatorial Chemistry» Angelo Agazzi and Laura Favretto, Milestone «MicroSynth microwave labstation for organic synthesis» Application Chris Mason and Steven P. Hailey, CEM Microwave Tech. «CEM gets on the leading edge of microwave synthesis» 10.00–11.00 Antonello Pessi, IRBM, P. Angeletti, Merck Rome, Pomezia (Italy) «Combinatorial Peptide Libraries and Drug Design: Human Hepatitis C as a case study» 16.00-16.45 Angela Comas and Rico Bongaarts, UnionBiometrica «Bead-based assays using CopasTM flow sorting» 11.00-11.30 Coffee break, Exhibits (room 57, 1st floor) 16.45-17.25 Marco Leggieri, Genevac «Key evaporation issue» 17.25-18.00 Stefano Giovanninetti, Stepbio-Argonaut «Parallel chromatography and purifications» 11.30-12.30 Elisabetta Bianchi, IRBM, P. Angeletti, Merck Rome, Pomezia (Italy) «Peptide Libraries with pre-defined conformations» 12.30-13.30 Anna Maria Papini, University of Florence (Italy) «A combinatorial approach for the rational design of innovative diagnostic tools for autoimmune diseases» 13.30–14.30 Lunch, Exhibits (room 57, 1st floor) 18.00-18.15 Maria Claudia Alcaro, ThermoFinnigan «ESI-MS characterization of the result of the synthesis performed during the practical sessions» Aula 186, Polo Scientifico, Via della Lastruccia 3, Sesto Fiorentino (FI) 18.30-19.00 Concluding remarks: “Arrivederci” Saturday, April 12TH 2003 SOCIAL EVENTS 9.30-12.00 Visiting tour in Florence and Uffizi Museum