RG1. Medicinal Chemistry ... back
The main goal of the group is the development of synthetic, analytical and theoretical tools to design small
molecules with medicinal and/or environmental importance.
In particular, specific aims are:
- Discovery and development of new target-based lead structures for single or combined therapy
- Development of green and sustainable synthetic processes
- Evaluation of drug-like properties of drug-candidates
- Evaluation of drug-drug and drug-metabolite interactions
- Design and synthesis of nanosystems for drug delivery and other applications
- Development of bio and chemoinformatic tools for computer assisted design
- Development of new analytical methodologies for implementation of in-house screening assays
The MedChem group is composed by a cross-functional team working at the chemistry–biology interface in R&D areas related to human health and well-being.The multidisciplinary and internationally recognized MedChem group areas of expertise are drug discovery, analysis and nanomedicine. The main goal of the MedChem group is the transfer of patented/patentable innovations for further development in the pharmaceutical/biotech industries.In this context, two patents «Hydroxycinnamic derivatives, methods and uses thereof» (PCT/IB2017/056412) and «Hydroxybenzoic derivatives, methods and uses thereof (PCT/IB2017/058508)» have been licensed to MitoTAG, a spin-off co-founded by RG1 Coordinator, that develops antioxidant mitochondria-targeting systems for cosmetics, human health and veterinary (http://www.mitotag.com/).
Research Group Team:
Coordinator: Fernanda Borges. Senior Researchers: Jorge Garrido; Manuela Garrido. Research Fellows: Fernando Cagide; Alexandra Gaspar; Maria João Matos
Postdoctoral Researchers: José Teixeira; Tiago Silva (with CNC); Catarina Oliveira; Sofia Benfeito; Carlos Fernandes; Filomena Silva (with CNC); Pedro Soares
PhD Students: Daniel Chavarria (with CNC); Daniel Martins; Lisa Sequeira; Miguel Pinto; Ricardo Amorim (with CNC); Joana Malheiro (with LEPABE); Diana Oliveira (with LEPABE); Francesco Mesiti (with University of Catanzaro, Italy); Maria Inês Simões (ETN Foie Gras)
Drug discovery and development of new therapeutic solutions for oxidative stress-related diseases, namely neurodegenerative diseases
The project embraces the discovery of new chemical entities acting as single or multitarget agents toward classic and non-classic targets of neurodegenerative diseases (Alzheimer’s Disease, Parkinson’s Disease and Amyotrophic Lateral Sclerosis). The project is supported by the network of two COST Actions- CM1406 Epigenetic Chemical Biology and CA15135 Multi-target paradigm for innovative ligand identification in the drug discovery process (MuTaLig) and by national projects, namely Mito4ALS - Development of Novel Mitochondria-Targeted Antioxidants for Improving SOD1-Familial Amyotrophic Lateral Sclerosis Phenotype (POCI-01-0145-FEDER-02939) and COMT4BRAIN-Development of centrally-active and safe catechol O-methyltransferase inhibitors (POCI-01-0145-FEDER-29164).
Drug discovery and development of new therapeutic solutions for liver diseases
The project is focused in discovery of new chemical entities for Non-Alcoholic Fatty Liver Disease (NAFLD), including its main pathologic outcome the non-alcoholic steatohepatitis (NASH). It was initiated in 2017 and is supported by two European projects (FOIE GRAS, H2020MSCA-ITN- Bioenergetic Remodeling in the Pathophysiology and Treatment of Non-Alcoholic Fatty Liver Disease and mtFOIE GRAS, MSCA-RISE- Non-invasive Profiling of Mitochondrial Function in Non-Alcoholic Fatty Liver Disease) and a national project PTDC/DTP-FTO/2433/2014- MitoBOOST: A Next-Generation Therapeutics for Non-Alcoholic Fatty Liver Disease Based on Smart Antioxidant Delivery to Mitochondria. The international and national networks assure the mandatory biological screenings and in vivo assays needed for the rational drug discovery project.
Drug discovery and development of new antimicrobial and/or antibiofilm agents
The project aims at discovering new antibacterial and/or antibiofilm agents (following one target or multitarget strategies) to fuel the antibacterial armamentarium. The project is based on an innovative drug discovery strategy based on privileged scaffolds and fragments, which is ahead from the me-too and me-better approaches used so far by pharmaceutical industry. To speed up the process, the group established collaborations with CO-ADD (Community for Open Antimicrobial Drug Discovery) and LEPABE research center. The project is also supported by the network of CA15135 Multi-target paradigm for innovative ligand identification in the drug discovery process (MuTaLig) and the national projects ABFish-Development of new antibiotics for aquaculture (POCI-01-0145-FEDER-028397) and BOFILM-Development of novel biocide solutions for effective biofilm control (POCI-01-0145-FEDER-030219).
Development of smart delivery systems to address selectivity, permeability, chemical/metabolic stability and/or toxicity shortcomings.
Despite research efforts to discover and develop effective and safe drugs, the majority of candidates fail in preclinical and clinical trials due to inadequate pharmacokinetics, namely water solubility and membrane permeability. These drawbacks can be solved using nanotechnology approaches, namely by the use of smart carrier systems based on polymers, sugars or cyclodextrins, among others.
The MedChem group is engaged in the development of nanomedicine innovative solutions using different nanocarriers and engineering micro- and nanoformulations. The project is sustained by strong collaborations with other national and international partnerships and by the European Technology Platform on Nanomedicine.