Detailed Programme

Wednesday, 23 November 2022

14:00 Platform opening
15:00–15:30
Opening of the Meeting

Session 1 – Structural aspects of drug design

Chairman: Višnja Stepanić

15:30–16:15
PL-1
Martin Smieško (University of Basel, Switzerland)
Designing Safer Drugs: Structure-Based Methods in Predicting Off-target Binding
16:15–16:35
L-1
Silvia Salerno (University of Pisa, Italy)
Indole-based derivatives as carbonic anhydrase activators for neurodegeneration diseases
16:35–17:20
PL-2
Peter Ertl (Novartis Institutes for BioMedical Research in Basel, Switzerland)
Magic Rings: Navigation in the Chemical Space of Bioactive Rings
17:20–17:40
L-2
Valeria Pittala (University of Catania, Italy)
Progress in the development of novel heme oxygenase-1 inhibitors with potent anti-proliferative activity


Thursday, 24 November 2022

Session 2 – New compounds in combating infectious diseases

Chairman: Gabriele Costantino

09:00–09:45
PL-3
Giannamaria Annunziato (University of Parma, Italy)
Dealing with anti-microbial resistance (AMR) by taking advantage of cysteine biosynthesis inhibitors as antimicrobial adjuvants
09:45–10:15
KL-1
Stella Maria Cascioferro (University of Palermo, Italy)
Anti-virulence agents with anti-biofilm mechanism of action to counteract antibiotic resistance in grampositive pathogens
     
10:15–10:45
Coffee break

Session 3 – Structural insights in new antibacterial drugs

Chairman: Michael Schnürch

10:45–11:30
PL-4
Jan Zitko (Charles University, Czechia)
Biological properties of pyrazinamide derivatives: Antimicrobial activity and beyond
11:30–12:00
KL-2
Katharina Pallitsch (University of Vienna, Austria)
Organic chemistry as a potent tool to study human metabolism
12:00–12:20
L-3
Azzurra Stefanucci (University “Gabriele d’Annunzio”, Italy)
Discovery of new teixobactin analogues with total lactam bridge
     
12:20–14:00
Lunch
14:00–15:00
Poster Session I (odd numbers)

Session 4 – Compounds with antiviral potency

Chairman: Jan Zitko

15:00–15:45
PL-5
Anikó Borbás (University of Debrecen, Hungary)
Emerging roles of glycopeptide antibiotics: teicoplanin and vancomycin derivatives with enhanced antibacterial and antiviral activities
15:45–16:05
L-4
Simona Musella (University of Salerno, Italy)
Rational design of the zonulin inhibitor AT1001 derivatives as potential SARS-COV-2 clinical candidates for intranasal administration
     
16:05–16:35
Coffee break

Session 5 – Searching for new targets for drug design

Chairman: Magdaléna Májeková

16:35–16:55
L-5
Arianna Gelain (University of Milan, Italy)
Development of a novel approach to overcome biofilm formation by natural product derivatives
16:55–17:15
L-6
Marta Giorgis (Turin University, Italy)
Important steps into drug development of MEDS433, a potent human dihydroorotate dehydrogenase inhibitor based on the 2-hydroxypyrazole[1,5-A] pyridine scaffold
17:15–17:35 L-8 Ana Penava (University of Zagreb, Croatia)
Synthesis of new generation of harmiquins, harmine and chloroquine hybrids as potential antiplasmodial agents


Friday, 25 November 2022

Session 6 – The role of organic chemistry in drug design I.

Chairman: Lucia Kováčiková

08:30–09:15
PL-6
Nela Malatesti (University of Rijeka, Croatia)
The tale of the lipophilic tail of the meso-tripyridinium porphyrins in the photodynamic action
09:15–09:45
KL-3
Sándor Balázs Király (University of Debrecen, Hungary)
Domino cyclization reactions for the preparation of condensed heterocycles with antiproliferative activity
     
09:45–10:15
Coffee break

Session 7 – Compounds for treatment of CNS disorders

Chairman: Dariusz Matosiuk

10:15–11:00
PL-7
Marcin Kolaczkowski (Jagiellonian University of Cracow, Poland)
Biased agonists of the 5-HT1A receptor – a new hope for addressing treatment-resistant depression?
11:00–11:30
KL-4
Slawomir Filipek (University of Warsaw, Poland)
Allosteric and ortho-allosteric modulation of G protein-coupled receptors
11:30–12:00
KL-5
Urban Košak (University of Ljubljana, Slovenia)
Selective inhibitors of butyrylcholinesterase for alleviating symptoms of Alzheimer’s disease
12:00–12:20 L-9 Halilibrahim Ciftci (Koc University, Istanbul, Turkey)
Development of next-generation drug candidates for ALS treatment
     
12:20–13:30
Lunch
13:30–14:30
Poster session II (even numbers)

Session 8 – The role of organic chemistry in drug design II.

Chairman: Peter Šramel

14:30–15:00
KL-6
Andrej Emanuel Cotman (University of Ljubljana, Slovenia)
Chiral going viral: Asymmetric catalysis paves the way for improved property lead compounds
15:00–15:30
KL-7
Đani Škalamera (University of Zagreb, Croatia)
Synthesis and immunoadjuvant activity of QS-7 analogs with truncated linear saccharide domain
15:30–15:50 L-10 Walter Kuba (TU Wien, Austria)
Boosting bioorthogonal bond-cleavage reactions of tetrazines and trans-cyclooctenes via intramolecular interactions
     
15:50–16:20
Coffee break

Session 9 – Specific targets in metabolic, CNS and inflammation disorders

Chairman: Marcin Kolaczkowski

16:20–16:50
KL-8
Milan Štefek (Slovak Academy of Sciences, Slovakia)
Novel indole-based bifunctional aldose reductase inhibitors/antioxidants as promising drugs for treatment of diabetic complications
16:50–17:20
KL-9
Tana Tandarić (University of Uppsala, Sweden & Ruder Boskovic Institute, Croatia)
An insight into the mechanism of the irreversible inhibition of monoamine oxidase enzymes by propargylamine inhibitors
17:20–17:40
L-11
Tania Ciaglia (University of Salerno, Italy)
New indoline-based 5-LOX/she dual inhibitors: in vitro and in vivo pharmacological characterization
17:40–18:00 L-12 Angela Corvino (University of Naples «Federico II», Italy)
Molecular hybrids between corticosteroids and H2S domains as a new therapeutic option for inflammatory disorders


Saturday, 26 November 2022

Session 10 – Structural aspects of ligand binding

Chairman: Emmanuel Mikros

09:00–09:45
PL-8
Marko Anderluh (University of Ljubljana, Slovenia)
Novel DNA gyrase inhibitors bind asymmetrically to their target using symmetrical bifurcated halogen bonds
09:45–10:15
KL-10
Josef Jampílek (Comenius University, Bratislava, Slovakia)
Investigations of new derivatives of β-hydroxyarylcarboxylic acids
10:15–10:45
KL-11
Dionysia Papagiannopoulou (University of Thessaloniki, Greece)
Technetium-99m tracers towards the development of molecular imaging agents
10:45–11:05
L-13
Gabriella La Spada (University of Bari Aldo Moro, Italy)
Structure-based design of phenyl ring bioisosteres: selectivity switch in dual AChE-MAO B and BChE-MAO B inhibitors
     
11:05–11:35
Coffee break

Session 11 – Perspective ligands for cancer treatment

Chairman: Marko Anderluh

11:35–11:55
L-14
Letizia Giampietro (University of Chieti-Pescara “G. d’Annunzio”, Italy)
New synthesized phenyldiazenyl sulphonamides as aromatase inhibitors
11:55–12:15
L-15
Veronica Di Sarno (University of Salerno, Italy)
TRPM8 antagonists as new potential therapeutics in castration-resistant prostate cancer (CRPC)
12:15–12:35 L-16 Maria Dichiara (Northeastern University, Boston, Massachusetts, USA)
Imidazopyridine derivatives for visceral Leishmaniasis: Synthesis and structure-property optimization
     
12:35–13:05
Winning Posters Flash presentations
13:05–13:35
Closing

 

Last update on 18 November 2022.

The programme might be subject to necessary changes.

 

MEETING SECRETARIAT
GUARANT International spol. s r. o.
Českomoravská 19, 190 00  Prague 9
Czech Republic
Phone: +420 284 001 444
E-mail: jmmc2022@guarant.cz