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Dr Michael Paradowski
Senior Research Fellow
- ParadowskiM@cardiff.ac.uk
- +44 29225 10847
- Main Building, Park Place, Cardiff, CF10 3AT
Overview
Michael has >20 year experience as a medicinal chemist in drug discovery, working for the pharmaceutical industry (Pfizer) and drug discovery groups within academia (University of Sussex, Cardiff University). Michael has extensive experience working across a range of target classes and disease areas encompassing anti-infectives, allergy & respiratory and CNS.
Michael is currently a Senior Research Scientist at Cardiff University where he was responsible for establishing the chemistry and biology laboratories at the Medicines Discovery Institute. Michael's current research interests are in CNS ion channels and in particular modulators of the GABAA receptors (Anxiety disorders, Neuropathic pain, Post-Partum depression, Psychosis, Epilepsy) where he is leading a portfolio of projects from early discovery to late stage pre-clinical studies.
Before joining the Medicines Discovery Institutes, Michael setup the research laboratories within the Sussex Drug Discovery group where he invented Sisunatovir (RV521), an inhibitor of respiratory syncytial virus
As a project leader for Pfizer, Michael led multiple global chemistry teams, both in-house and externally to enable delivery of molecules from hit-to-lead through to candidate molecule scale up to support Phase 1 studies and has been involved in the discovery of Maraviroc and numerous Phase I and II clinical candidates
Michael graduated from the French Grandes Ecoles d'ingénieurs ENSI Caen and holds a Ph.D. in Chemistry from the University of Sussex and is author and inventor on multiple patents and publications
Publication
2021
- Cockerill, G. S. et al. 2021. Discovery of sisunatovir (RV521), an inhibitor of respiratory syncytial virus fusion. Journal of Medicinal Chemistry 64(7), pp. 3658-3676. (10.1021/acs.jmedchem.0c01882)
2019
- Beswick, P. et al. 2019. A challenge finding P2X1 and P2X4 ligands. Neuropharmacology 157, pp. 107674. (10.1016/j.neuropharm.2019.107674)
2017
- West, R. A. et al. 2017. African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase. European Journal of Medicinal Chemistry 141, pp. 676-689. (10.1016/j.ejmech.2017.09.067)
2016
- Hornyak, P. et al. 2016. Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2. Biochemical Journal 473(13), pp. 1869-1879. (10.1042/BCJ20160180)
- Cockerill, S., Mathews, N., Ward, S., Lunn, G., Paradowski, M. and Gascon Simorte, J. M. 2016. Spiro-indolines for the treatment and prophylaxis of respiratory syncytial virus infection (RSV). WO2016055780A1 [Patent].
- Moore, T. O., Paradowski, M. and Ward, S. 2016. An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C-H activation. Organic and Biomolecular Chemistry 14(12), pp. 3307-3313. (10.1039/C6OB00340K)
2014
- Wakenhut, F. et al. 2014. The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile—part 2. ChemMedChem 9(7), pp. 1387-1396. (10.1002/cmdc.201400046)
- Tran, T. D. et al. 2014. The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile-Part 1. ChemMedChem 9(7), pp. 1378-1386. (10.1002/cmdc.201400045)
2013
- Burrows, A. D. et al. 2013. Incorporation by coordination and release of the iron chelator drug deferiprone from zinc-based metal-organic frameworks. Chemical Communications 49(96), pp. 11260-11262. (10.1039/c3cc45689g)
2012
- Lane, C. A., Hay, D., Mowbray, C. E., Paradowski, M., Selby, M. D., Swain, N. A. and Williams, D. H. 2012. Synthesis of novel histamine H4 receptor antagonists. Bioorganic and Medicinal Chemistry Letters 22(2), pp. 1156-1159. (10.1016/j.bmcl.2011.11.098)
2011
- Egan, B. A., Paradowski, M., Thomas, L. H. and Marquez, R. 2011. http://dx.doi.org/10.1016/j.tet.2011.10.036. Tetrahedron 67(50), pp. 9700-9707. (10.1016/j.tet.2011.10.036)
- Hay, D. A. et al. 2011. A flexible synthesis of C-6 and N-1 analogues of a 4-amino-1,3-dihydroimidazo[4,5-c]pyridin-2-one core. Tetrahedron Letters 52(44), pp. 5728-5732. (10.1016/j.tetlet.2011.08.119)
- Mowbray, C. E. et al. 2011. Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: A novel histamine H4 receptor antagonist. Bioorganic and Medicinal Chemistry Letters 21(21), pp. 6596-6602. (10.1016/j.bmcl.2011.07.125)
- Adam, F. M. et al. 2011. Development of a practical synthesis of toll-like receptor agonist PF-4171455: 4-Amino-1-benzyl-6-trifluoromethyl-1,3-dihydroimidazo [4,5-c] pyridin-2-one. Organic Process Research and Development 15(4), pp. 788-796. (10.1021/op200021a)
- Egan, B. A., Paradowski, M., Thomas, L. H. and Marquez, R. 2011. Regiocontrolled rearrangement of isobenzofurans. Organic Letters 13(8), pp. 2086-2089. (10.1021/ol200498k)
- Paradowski, M., Lane, C. and Peakman, T. 2011. Synthesis of a Novel Octahydro Pyrrolo[3,4-c]pyrrole Cyclic Amidine via 1,3-Dipolar Cycloaddition of Azomethine Ylides. SYNLETT 2011(11), pp. 1543-1546. (10.1055/s-0030-1260768)
- Pryde, D. C. et al. 2011. The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection. MedChemComm 2(3), pp. 185. (10.1039/C0MD00197J)
Erthyglau
- Cockerill, G. S. et al. 2021. Discovery of sisunatovir (RV521), an inhibitor of respiratory syncytial virus fusion. Journal of Medicinal Chemistry 64(7), pp. 3658-3676. (10.1021/acs.jmedchem.0c01882)
- Beswick, P. et al. 2019. A challenge finding P2X1 and P2X4 ligands. Neuropharmacology 157, pp. 107674. (10.1016/j.neuropharm.2019.107674)
- West, R. A. et al. 2017. African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase. European Journal of Medicinal Chemistry 141, pp. 676-689. (10.1016/j.ejmech.2017.09.067)
- Hornyak, P. et al. 2016. Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2. Biochemical Journal 473(13), pp. 1869-1879. (10.1042/BCJ20160180)
- Moore, T. O., Paradowski, M. and Ward, S. 2016. An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C-H activation. Organic and Biomolecular Chemistry 14(12), pp. 3307-3313. (10.1039/C6OB00340K)
- Wakenhut, F. et al. 2014. The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile—part 2. ChemMedChem 9(7), pp. 1387-1396. (10.1002/cmdc.201400046)
- Tran, T. D. et al. 2014. The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile-Part 1. ChemMedChem 9(7), pp. 1378-1386. (10.1002/cmdc.201400045)
- Burrows, A. D. et al. 2013. Incorporation by coordination and release of the iron chelator drug deferiprone from zinc-based metal-organic frameworks. Chemical Communications 49(96), pp. 11260-11262. (10.1039/c3cc45689g)
- Lane, C. A., Hay, D., Mowbray, C. E., Paradowski, M., Selby, M. D., Swain, N. A. and Williams, D. H. 2012. Synthesis of novel histamine H4 receptor antagonists. Bioorganic and Medicinal Chemistry Letters 22(2), pp. 1156-1159. (10.1016/j.bmcl.2011.11.098)
- Egan, B. A., Paradowski, M., Thomas, L. H. and Marquez, R. 2011. http://dx.doi.org/10.1016/j.tet.2011.10.036. Tetrahedron 67(50), pp. 9700-9707. (10.1016/j.tet.2011.10.036)
- Hay, D. A. et al. 2011. A flexible synthesis of C-6 and N-1 analogues of a 4-amino-1,3-dihydroimidazo[4,5-c]pyridin-2-one core. Tetrahedron Letters 52(44), pp. 5728-5732. (10.1016/j.tetlet.2011.08.119)
- Mowbray, C. E. et al. 2011. Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: A novel histamine H4 receptor antagonist. Bioorganic and Medicinal Chemistry Letters 21(21), pp. 6596-6602. (10.1016/j.bmcl.2011.07.125)
- Adam, F. M. et al. 2011. Development of a practical synthesis of toll-like receptor agonist PF-4171455: 4-Amino-1-benzyl-6-trifluoromethyl-1,3-dihydroimidazo [4,5-c] pyridin-2-one. Organic Process Research and Development 15(4), pp. 788-796. (10.1021/op200021a)
- Egan, B. A., Paradowski, M., Thomas, L. H. and Marquez, R. 2011. Regiocontrolled rearrangement of isobenzofurans. Organic Letters 13(8), pp. 2086-2089. (10.1021/ol200498k)
- Paradowski, M., Lane, C. and Peakman, T. 2011. Synthesis of a Novel Octahydro Pyrrolo[3,4-c]pyrrole Cyclic Amidine via 1,3-Dipolar Cycloaddition of Azomethine Ylides. SYNLETT 2011(11), pp. 1543-1546. (10.1055/s-0030-1260768)
- Pryde, D. C. et al. 2011. The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection. MedChemComm 2(3), pp. 185. (10.1039/C0MD00197J)
Patentau
- Cockerill, S., Mathews, N., Ward, S., Lunn, G., Paradowski, M. and Gascon Simorte, J. M. 2016. Spiro-indolines for the treatment and prophylaxis of respiratory syncytial virus infection (RSV). WO2016055780A1 [Patent].
Research
Michael's current research interests are in CNS ion channels and in particular modulators of the GABAA receptors (Anxiety disorders, Neuropathic pain, Post-Partum depression, Psychosis, Epilepsy)
Project Leader for MRC funded non-sedating anxiolytic a2/3-GABA subtype selective modulator
Project leader for Wellcome Trust Innovator Award: Developing small molecules as a neurosteroid replacement strategy for treating postpartum psychosis
Biography
Michael has >20 year experience as a medicinal chemist in drug discovery, working for the pharmaceutical industry (Pfizer) and drug discovery groups within academia (University of Sussex, Cardiff University). Michael has extensive experience working across a range of target classes and disease areas encompassing anti-infectives, allergy & respiratory and CNS.
Michael is currently a Senior Research Scientist at Cardiff University where he was responsible for establishing the chemistry and biology laboratories at the Medicines Discovery Institute. Michael's current research interests are in CNS ion channels and in particular modulators of the GABAA receptors (Anxiety disorders, Neuropathic pain, Post-Partum depression, Psychosis, Epilepsy) where he is leading a portfolio of projects from early discovery to late stage pre-clinical studies.
Before joining the Medicines Discovery Institutes, Michael setup the research laboratories within the Sussex Drug Discovery group where he invented Sisunatovir (RV521), an inhibitor of respiratory syncytial virus
As a project leader for Pfizer, Michael led multiple global chemistry teams, both in-house and externally to enable delivery of molecules from hit-to-lead through to candidate molecule scale up to support Phase 1 studies and has been involved in the discovery of Maraviroc and numerous Phase I and II clinical candidates
Michael graduated from the French Grandes Ecoles d'ingénieurs ENSI Caen and holds a Ph.D. in Chemistry from the University of Sussex and is author and inventor on multiple patents and publications