Cedric Stephan Graebin

Cedric Stephan Graebin
University of Dundee · Division of Biological Chemistry and Drug Discovery

Doctor of Philosophy

About

34
Publications
14,571
Reads
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446
Citations
Introduction
Cedric Stephan Graebin is a Medicinal Chemistry Trainer at the Wellcome Centre for Anti-Infectives Research at the University of Dundee, Scotland. His main focus is on the training and dissemination of medicinal chemistry-related knowledge concerning the development of new drugs for neglected diseases.
Additional affiliations
February 2022 - present
University of Dundee
Position
  • Medicinal Chemistry Trainer
Description
  • As a Medicinal Chemistry Trainer within the Wellcome Centre for Anti-Infectives Research (WCAIR), the focus is on the dissemination of Medicinal Chemistry-related knowledge for trainees coming from all over the world concerning the search of novel anti-infective agents for neglected diseases.
November 2009 - January 2022
Federal Rural University of Rio de Janeiro
Position
  • Professor
Description
  • Medicinal Chemistry, focusing on the design and development of new bioactive compounds
Education
March 2004 - December 2008
Universidade Federal do Rio Grande do Sul
Field of study
  • Pharmaceutical Sciences
May 1999 - August 2003
Universidade Federal do Rio Grande do Sul
Field of study
  • Pharmaceutical Sciences

Publications

Publications (34)
Article
Cardiovascular diseases (CVDs) comprise a group of diseases and disorders of the heart and blood vessels, which together are the number one cause of death worldwide, being associated with multiple genetic and modifiable risk factors, and that may directly arise from different etiologies. For a long time, the search for cardiovascular drugs was base...
Article
Neglected tropical diseases are a diverse group of communicable diseases that are endemic in low- or low-to-middle-income countries located in tropical and subtropical zones. The number and availability of drugs for treating these diseases are low, the administration route is inconvenient in some cases, and most of them have safety, efficacy, or ad...
Article
Cyclic nucleotide phosphodiesterases (PDEs) are a superfamily of enzymes known to play a critical role in the indirect regulation of several intracellular metabolism pathways through the selective hydrolysis of the phosphodiester bonds of specific second messenger substrates such as cAMP (3',5'-cyclic adenosine monophosphate) and cGMP (3',5'-cyclic...
Article
Introduction: In this work DHPMs were combined with the quinoline nucleus to obtain new quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione compounds with improved antiplasmodial activity as well as decreased cytotoxicity. Nineteen quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione derivatives connected by a linker group to quinolone ring moieties with diffe...
Article
Full-text available
DOI: 10.2174/1570179416666190718153703 Multicomponentreactions (MCRs) are composed from three or more reagents in which the final product has all or most of the carbon atoms from its starting materials.These reactions represent, in the Medicinal Chemistry context, a great potential in the research for new bioactive compounds, since their productsc...
Article
Full-text available
Background: Malaria is responsible for 429,000 per year deaths worldwide with more than 200 million cases reported in 2015. Increasing parasite resistance has been imposing restrictions to the currently available antimalarial drugs. Thus, the search for new effective and safe antimalarial drugs is therefore crucial in the current scenario. Heterocy...
Chapter
Glycyrrhizin or, more correctly, Glycyrrhizinic acid is a triterpenoid saponin obtained from the root and rhizome extracts of Licorice (Glycyrrhiza glabra), being commonly used as a sweetener, being reported as – at least – 30 times sweeter than sucrose. This natural product, along with its aglycone glycyrrhetinic acid, is known in the literature f...
Article
Full-text available
Microtubules play critical roles in vital cell processes, including cell growth, division, and migration. Microtubule-targeting small molecules are chemotherapeutic agents that are widely used in the treatment of cancer. Many of these compounds are structurally complex natural products (e.g., paclitaxel, vinblastine, and vincristine) with multiple...
Data
Synthesis and drug design approach. (PDF)
Data
Structures of the tubulin target agents: colchicine, paclitaxel, vinblastine, vincristine, combretastatin A-4 and podophyllotoxin. (PDF)
Data
Synthetic procedures and compound characterization. (DOCX)
Article
Full-text available
Multicomponent reactions (MCRs) are reactions that start from three or more reagents in order to obtain only one final product that has all or most of the carbon atoms from its starting materials. Regarding the Green Chemistry goals, MCRs emerge as ideal processes, with its atomic economy and less waste, as well as being tools for the creation of w...
Article
Full-text available
A series of 3,4-dihydropyrimidin-2(1H)-one/thione (IV), (VI), (VIII) with high UV absorption and blue fluorescent properties are synthesized from synthetic coumarin β-ketoester derivatives.
Article
Full-text available
The optimization of a Biginelli Multicomponent Reaction (MCR) protocol for obtaining a collection of 3,4-dihydropyrimidin-2(1H)-one/thione, with UV absorption and blue fluorescent properties, from synthetic coumarin beta-ketoester derivatives is described. This is the first report of Biginelli adducts bearing a coumarin nucleus in the β-ketoester m...
Article
Full-text available
The aerial parts of Ipomoea batatas are described herein to produce four new resin glycosides, designated as ipomotaosides A, B, C, and D. Ipomotaoside A was found to present inhibitory activity on both cyclooxygenases. However, the conformational elucidation of these molecules may be difficult due to their high flexibility. In this context, the cu...
Article
Glycyrrhizin, a saponin, and its aglicone Glycyrrhetinic acid are natural products found in the Liquorice (Glycyrrhyza glabra L.) root extract. This saponin is known for its in vitro and in vivo Thrombin inhibitory activity. The design and synthesis of five glycyrrhizin derivatives was carried out in order to improve the natural product activity. C...
Article
Full-text available
Background The discovery and development of anti-malarial compounds of plant origin and semisynthetic derivatives thereof, such as quinine (QN) and chloroquine (CQ), has highlighted the importance of these compounds in the treatment of malaria. Ursolic acid analogues bearing an acetyl group at C-3 have demonstrated significant anti-malarial activit...
Article
Full-text available
The development of hybrid compounds containing limonene-and recognized anti-T. cruzi-heterocycle-frameworks is described. The six new compounds displayed broad antitrypanosomal activities having 5-nitrofuran and 5-nitroindazole derivatives, the best profiles. In addition, a 5-nitroindazole derivative evaluated against a panel of fungi ex-hibited re...
Article
The synthesis and in vitro activity of R(+)-Limonene derivatives against Leishmania and Trypanosoma cruzi strains are reported. Seven compounds have shown better in vitro activity against Leishmania (V.)braziliensis than the standard drug pentamidine. Additionally, we have identified two promising new anti-T. cruzi limonene derivatives.
Article
Full-text available
Neste trabalho nós apresentamos uma revisão sobre a síntese em fase sólida de metabólitos secundários, tais como alcalóides, poliaminas, esteróides, terpenos e flavonóides, descritos na literatura a partir de 2000. Um número considerável de rotas sintéticas elegantes e desafiadoras, usando suportes sólidos, será discutido. In this manuscript, we di...
Article
Full-text available
O ácido glicirrizínico (GL), também conhecido como glicirrizina, é uma saponina triterpênica, um produto natural encontrado na raiz de Glycyrrhyza glabra L. ("licquorice" ou "alcaçuz"), utilizada mundialmente como edulcorante e também na medicina tradicional do Oriente. Este artigo de revisão enfoca os novos compostos sintetizados usando GL ou sua...
Article
Full-text available
The therapy of parasitic diseases has relied, until recently, on the use of a very limited number of drugs, most of them of low efficacy, leading to side effects and in certain cases with high toxicity. This review focuses on the chemother-apy to treat diseases caused by Trypanosoma cruzi (Chagas' disease), Trypanosoma b. gambiense and Trypanosoma...
Article
Full-text available
A series of seven limonene beta-amino alcohol derivatives has been regioselectively synthesised in moderate to good yields. Two of these compounds were found to be significantly effective against in vitro cultures of the Leishmania (Viannia) braziliensis promastigote form in the micromolar range. The activities found for 3b and 3f were about 100-fo...
Article
In this work, we were able to synthesize, in good isolated yields, seven R(+)-limonene derived amines (five of that described for the first time) employing a rhodium catalysed hydroaminomethylation reaction. This protocol consists in an one-pot three step reaction: double bond hydroformylation, aldehyde/amine condensation and imine/enamine hydrogen...
Article
Full-text available
"Syntheis and In Vivo Assay of Indometacin Esters as a Medicinal Chemistry Practical Class for Graduate Students". This article shows a Medicinal Chemistry practical class, created and developed by students of the Pharmaceutical Sciences Post-Graduate Program (PPGCF/UFRGS). It describes the planning, synthesis and in vivo biological evaluation of f...
Article
Full-text available
Solid-phase organic synthesis (SPOS) has been considered the main strategy for the construction of combinatorial libraries, because its simplicity leads to faster synthetic procedures. In addition to that, a series of reports in the specialized literature show great advantages in the use of microwave activation, when compared to classical heating,...
Article
Full-text available
Solid-phase organic synthesis (SPOS) has been considered the main strategy for the construction of combinatorial libraries, because its simplicity leads to faster synthetic procedures. In addition to that, a series of reports in the specialized literature show great advantages in the use of microwave activation, when compared to classical heating,...
Article
Full-text available
The use of KBr pellets in infrared spectroscopy has been investigated for monitoring solid-phase reactions. Synthesis of the methyl p-aminobenzoate on Merrifield resin (MR) is described as a model for this technique, which allows the progress of its three on-bead reaction steps to be monitored throughout their duration.

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Projects

Projects (3)
Project
Glycyrrhizin or, more correctly, Glycyrrhizinic acid, is a triterpene saponin found in the root extract of Liquorice, presenting several relevant biologic activities. This project aims to improve the weak allosteric thrombin inhibitory activity of Glycyrrhizin through the design and development of semi-synthetic or synthetic compounds inspired in the triterpene scaffold.
Project
Multicomponent reactions (MCRs) are reactions that start from three or more reagents in order to obtain only one final product that has all or most of the carbon atoms from its starting materials. This project aims to discover and develop new bioactive compounds employing multicomponent reactions (such as Biginelli, Hantzsch, Mannich and Ugi protocols).