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Rui Moreira

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Chemicals & Drugs

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Susana D Lucas; Elsa Costa; Rita C Guedes; Rui Moreira
Targeting COPD: advances on low-molecular-weight inhibitors of human neutrophil elastase.
Daniela M Santos; Maria M M Santos; Susana Solá; Rui Moreira; Cecília M P Rodrigues
Synthetic condensed 1,4-naphthoquinone derivative shifts neural stem cell differentiation by regulating redox state.
L F Rocha e Silva; Wanderli Pedro Tadei; R S Zacardi; R C N Amorim; V F Andrade Neto; D S Costa; M R F Costa; G Dantas; M N Eberlin; M C Henrique; J Lavrado; M R Melo; A Montoia; Rui Moreira; S M Nunomura; Alexandra Paulo; A C Pinto; A M Pohlit
Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ellipticine, olivacine, cryptolepine and a synthetic cryptolepine analog.

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All Publications

2013: Susana D Lucas; Elsa Costa; Rita C Guedes; Rui Moreira
Targeting COPD: advances on low-molecular-weight inhibitors of human neutrophil elastase.
Medicinal research reviews 2013;33 Suppl 1():E73-E101.
2013: Daniela M Santos; Maria M M Santos; Susana Solá; Rui Moreira; Cecília M P Rodrigues
Synthetic condensed 1,4-naphthoquinone derivative shifts neural stem cell differentiation by regulating redox state.
Molecular neurobiology 2013;47(1):313-24.
2012: L F Rocha e Silva; Wanderli Pedro Tadei; R S Zacardi; R C N Amorim; V F Andrade Neto; D S Costa; M R F Costa; G Dantas; M N Eberlin; M C Henrique; J Lavrado; M R Melo; A Montoia; Rui Moreira; S M Nunomura; Alexandra Paulo; A C Pinto; A M Pohlit
Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ellipticine, olivacine, cryptolepine and a synthetic cryptolepine analog.
Phytomedicine : international journal of phytotherapy and phytopharmacology 2012;20(1):71-6.
2012: Sílvia Vale-Costa; Paula Gomes; Joana Matos; Rui Moreira; Ana M Tomás; Nuno Vale; Maria Salomé Gomes
Peptidomimetic and organometallic derivatives of primaquine active against Leishmania infantum.
Antimicrobial agents and chemotherapy 2012;56(11):5774-81.
2012: João Lavrado; Zachary Mackey; James H McKerrow; Elizabeth Hansell; Alexandra Paulo; Rui Moreira
Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives.
Bioorganic & medicinal chemistry letters 2012;22(19):6256-60.
2012: Ana Bela Santana; Teresa A F Cardote; Henrique F Correia; Lídia M Gonçalves; Rita C Guedes; Jim Iley; Susana D Lucas; Rui Moreira
N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.
Bioorganic & medicinal chemistry letters 2012;22(12):3993-7.
2012: Filipa P da Cruz; Francisco-Javier Gamo; Michael Hannus; Maria J Lafuente-Monasterio; Matthias Marti; Cécilie Martin; Rui Moreira; Maria M Mota; Tiago Rodrigues; Birte soennichsen; Kathrin Buchholz; Miguel Prudêncio
Drug screen targeted at Plasmodium liver stages identifies a potent multistage antimalarial drug.
The Journal of infectious diseases 2012;205(8):1278-86.
2012: Nuno Vale; Iva Fernandes; Nuno Mateus; Rui Moreira; Paula Gomes
Comparative analysis of in vitro rat liver metabolism of the antimalarial primaquine and a derived imidazoquine.
Drug metabolism letters 2012;6(1):15-25.
2012: João Lavrado; Elena Bichenkova; Kenneth T Douglas; Alexandra Paulo; Rui Moreira
1H NMR spectroscopic identification of protonable sites in cryptolepines with C-11 substituents containing two amino functionalities.
Magnetic resonance in chemistry : MRC 2012;50(3):216-20.
2012: Tiago Rodrigues; Rui Moreira; Maria M Mota; Miguel Prudêncio; Francisca Lopes
Targeting the liver stage of malaria parasites: a yet unmet goal.
Journal of medicinal chemistry 2012;55(3):995-1012.
2012: Graça Mata; Luis Constantino; Virgílio E do Rosário; Jim Iley; Rui Moreira
A carbamate-based approach to primaquine prodrugs: antimalarial activity, chemical stability and enzymatic activation.
Bioorganic & medicinal chemistry 2012;20(2):886-92.
2011: Paulo M C Glória; Lídia M Gonçalves; Jiri Gut; Rui Moreira; Philip J Rosenthal; Maria M M Santos
Aza vinyl sulfones: synthesis and evaluation as antiplasmodial agents.
Bioorganic & medicinal chemistry 2011;19(24):7635-42.
2011: Tiago Rodrigues; Philip J Rosenthal; Giancarlo A Biagini; Daniel J V A dos Santos; Jiri Gut; Francisca Lopes; Rui Moreira; Paul M O Neill; Rita C Guedes
Identification of new antimalarial leads by use of virtual screening against cytochrome bc₁.
Bioorganic & medicinal chemistry 2011;19(21):6302-8.
2011: Rita Capela; Jiri Gut; Francisca Lopes; Rui Moreira; Maria M Mota; Ghislain G Cabal; Philip J Rosenthal; Miguel Prudêncio
Design and evaluation of primaquine-artemisinin hybrids as a multistage antimalarial strategy.
Antimicrobial agents and chemotherapy 2011;55(10):4698-706.
2011: Sìlvia G Estácio; Rui Moreira; Rita C Guedes
Characterizing the dynamics and ligand-specific interactions in the human leukocyte elastase through molecular dynamics simulations.
Journal of chemical information and modeling 2011;51(7):1690-702.
2011: Paulo M C Glória; Isabel Coutinho; Lídia M Gonçalves; Cristina Baptista; Joana Soares; Ana S Newton; Rui Moreira; Lucília Saraiva; Maria M M Santos
Aspartic vinyl sulfones: inhibitors of a caspase-3-dependent pathway.
European journal of medicinal chemistry 2011;46(6):2141-6.
2011: Jalmira Mulchande; Sandra I Simões; Maria M Gaspar; Carla V Eleutério; Rudi Oliveira; Maria E M Cruz; Rui Moreira; Jim Iley
Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-β-lactam inhibitor of human leukocyte elastase.
Journal of enzyme inhibition and medicinal chemistry 2011;26(2):169-75.
2011: S Praveen Kumar; Jiri Gut; Rita C Guedes; Philip J Rosenthal; Maria M M Santos; Rui Moreira
Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials.
European journal of medicinal chemistry 2011;46(3):927-33.
2011: João Lavrado; Rui Moreira; Maria M Mota; Elena Bichenkova; Ghislain G Cabal; Cecília Díaz; Daniel J V A dos Santos; Kenneth T Douglas; Rita C Guedes; Jiri Gut; Miguel Prudêncio; Philip J Rosenthal; Alexandra Paulo
Incorporation of basic side chains into cryptolepine scaffold: structure-antimalarial activity relationships and mechanistic studies.
Journal of medicinal chemistry 2011;54(3):734-50.
2011: Tiago Rodrigues; Rui Moreira; Francisca Lopes
New hope in the fight against malaria?
Future medicinal chemistry 2011;3(1):1-3.
2010: João Lavrado; Anthony P Reszka; Rui Moreira; Stephen Neidle; Alexandra Paulo
C-11 diamino cryptolepine derivatives NSC748392, NSC748393, and NSC748394: anticancer profile and G-quadruplex stabilization.
Bioorganic & medicinal chemistry letters 2010;20(23):7042-5.
2010: João Lavrado; Kaamil Gani; Pedro A Nobre; Sofia A Santos; Paula Figueiredo; Dinora Lopes; Virgílio do Rosário; Jiri Gut; Philip J Rosenthal; Rui Moreira; Alexandra Paulo
Bis-alkylamine quindolone derivatives as new antimalarial leads.
Bioorganic & medicinal chemistry letters 2010;20(19):5634-7.
2010: Ana S Newton; Paulo M C Glória; Lídia M Gonçalves; Daniel J V A dos Santos; Rui Moreira; Rita C Guedes; Maria M M Santos
Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study.
European journal of medicinal chemistry 2010;45(9):3858-63.
2010: Jalmira Mulchande; Rudi Oliveira; Marta Carrasco; Luís Gouveia; Rita C Guedes; Jim Iley; Rui Moreira
4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.
Journal of medicinal chemistry 2010;53(1):241-53.
2010: Rui E Castro; Maria M M Santos; Paulo M C Glória; Carlos J A Ribeiro; Duarte M S Ferreira; Joana M Xavier; Rui Moreira; Cecília M P Rodrigues
Cell death targets and potential modulators in Alzheimer's disease.
Current pharmaceutical design 2010;16(25):2851-64.
2010: J Lavrado; Rui Moreira; Alexandra Paulo
Indoloquinolines as scaffolds for drug discovery.
Current medicinal chemistry 2010;17(22):2348-70.
2010: Tiago Rodrigues; F Lopes; Rui Moreira
Inhibitors of the mitochondrial electron transport chain and de novo pyrimidine biosynthesis as antimalarials: The present status.
Current medicinal chemistry 2010;17(10):929-56.
2010: Maria M M Santos; Natália Faria; Jim Iley; Simon J Coles; Michael B Hursthouse; M Luz Martins; Rui Moreira
Reaction of naphthoquinones with substituted nitromethanes. Facile synthesis and antifungal activity of naphtho[2,3-d]isoxazole-4,9-diones.
Bioorganic & medicinal chemistry letters 2010;20(1):193-5.
2009: Iva Fernandes; Nuno Vale; Victor de Freitas; Rui Moreira; Nuno Mateus; Paula Gomes
Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine.
Bioorganic & medicinal chemistry letters 2009;19(24):6914-7.
2009: Nuno Vale; Miguel Prudêncio; Catarina de Almeida Marques; Margaret S Collins; Jiri Gut; Fátima Nogueira; Joana Matos; Philip J Rosenthal; Melanie T Cushion; Virgílio E do Rosário; Maria M Mota; Rui Moreira; Paula Gomes
Imidazoquines as antimalarial and antipneumocystis agents.
Journal of medicinal chemistry 2009;52(23):7800-7.
2009: M Jesus Perry; Eduarda Mendes; Ana Luísa Simplício; Ana Coelho; Ricardo V Soares; Jim Iley; Rui Moreira; Ana Paula Francisco
Dopamine- and tyramine-based derivatives of triazenes: activation by tyrosinase and implications for prodrug design.
European journal of medicinal chemistry 2009;44(8):3228-34.
2009: Daniela M Santos; Maria M M Santos; Ricardo J S Viana; Rui E Castro; Rui Moreira; Cecília M P Rodrigues
Naphtho[2,3-d]isoxazole-4,9-dione-3-carboxylates: potent, non-cytotoxic, antiapoptotic agents.
Chemico-biological interactions 2009;180(2):175-82.
2009: Tiago Rodrigues; Rita C Guedes; Daniel J V A dos Santos; Marta Carrasco; Jiri Gut; Philip J Rosenthal; Rui Moreira; Francisca Lopes
Design, synthesis and structure-activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials.
Bioorganic & medicinal chemistry letters 2009;19(13):3476-80.
2009: Rita Capela; Rudi Oliveira; Lídia M Gonçalves; Ana Domingos; Jiri Gut; Philip J Rosenthal; Francisca Lopes; Rui Moreira
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition.
Bioorganic & medicinal chemistry letters 2009;19(12):3229-32.
2009: Nuno Vale; Fátima Nogueira; Virgílio E do Rosário; Paula Gomes; Rui Moreira
Primaquine dipeptide derivatives bearing an imidazolidin-4-one moiety at the N-terminus as potential antimalarial prodrugs.
European journal of medicinal chemistry 2009;44(6):2506-16.
2009: Cledir R Santos; Rita Capela; Cláudia S G P Pereira; Emília Valente; Luís Gouveia; Christophe Pannecouque; Erik De Clercq; Rui Moreira; Paula Gomes
Structure-activity relationships for dipeptide prodrugs of acyclovir: implications for prodrug design.
European journal of medicinal chemistry 2009;44(6):2339-46.
2009: Nuno Vale; Rui Moreira; Paula Gomes
Primaquine revisited six decades after its discovery.
European journal of medicinal chemistry 2009;44(3):937-53.
2009: Nuno Vale; Joana Matos; Rui Moreira; Paula Gomes
Electrospray ionization mass spectrometry as a valuable tool in the characterization of novel primaquine peptidomimetic derivatives.
European journal of mass spectrometry (Chichester, England) 2009;15(5):627-40.
2008: Nuno Vale; Joana Matos; Rui Moreira; Paula Gomes
Electrospray ionization-ion trap mass spectrometry study of PQAAPro and PQProAA mimetic derivatives of the antimalarial primaquine.
Journal of the American Society for Mass Spectrometry 2008;19(10):1476-90.
2008: Nuno Vale; Joana Matos; Jiri Gut; Fátima Nogueira; Virgílio E do Rosário; Philip J Rosenthal; Rui Moreira; Paula Gomes
Imidazolidin-4-one peptidomimetic derivatives of primaquine: synthesis and antimalarial activity.
Bioorganic & medicinal chemistry letters 2008;18(14):4150-3.
2008: Tiago Rodrigues; Rui Moreira; Rita C Guedes; Jim Iley; Francisca Lopes
Unanticipated acyloxymethylation of sumatriptan indole nitrogen atom and its implications in prodrug design.
Archiv der Pharmazie 2008;341(6):344-50.
2008: Cledir Santos; José Morais; Luis Filipe Gouveia; Erik De Clercq; Christophe Pannecouque; Carsten Uhd Nielsen; Bente Steffansen; Rui Moreira; Paula Gomes
Dipeptide derivatives of AZT: synthesis, chemical stability, activation in human plasma, hPEPT1 affinity, and antiviral activity.
ChemMedChem 2008;3(6):970-8.
2008: Jalmira Mulchande; Rita C Guedes; Wing-Yin Tsang; Michael I Page; Rui Moreira; Jim Iley
Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.
Journal of medicinal chemistry 2008;51(6):1783-90.
2008: A Martinelli; Rui Moreira; P V L Ravo
Malaria combination therapies: advantages and shortcomings.
Mini reviews in medicinal chemistry 2008;8(3):201-12.
2008: João Lavrado; Alexandra Paulo; Jiri Gut; Philip J Rosenthal; Rui Moreira
Cryptolepine analogues containing basic aminoalkyl side-chains at C-11: synthesis, antiplasmodial activity, and cytotoxicity.
Bioorganic & medicinal chemistry letters 2008;18(4):1378-81.
2008: Nuno Vale; Margaret S Collins; Jiri Gut; Ricardo Ferraz; Philip J Rosenthal; Melanie T Cushion; Rui Moreira; Paula Gomes
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones.
Bioorganic & medicinal chemistry letters 2008;18(2):485-8.
2007: Maria M M Santos; Rui Moreira
Michael acceptors as cysteine protease inhibitors.
Mini reviews in medicinal chemistry 2007;7(10):1040-50.
2007: Jalmira Mulchande; Luisa Martins; Rui Moreira; Margarida Archer; Tania F Oliveira; Jim Iley
The efficiency of C-4 substituents in activating the beta-lactam scaffold towards serine proteases and hydroxide ion.
Organic & biomolecular chemistry 2007;5(16):2617-26.
2007: Claudia Valente; Rui Moreira; Rita C Guedes; Jim Iley; Mohammed Jaffar; Kenneth T Douglas
The 1,4-naphthoquinone scaffold in the design of cysteine protease inhibitors.
Bioorganic & medicinal chemistry 2007;15(15):5340-50.
2007: Ricardo Ferraz; José Gomes; Eliandre de Oliveira; Rui Moreira; Paula Gomes
Unanticipated stereoselectivity in the reaction of primaquine alpha-aminoamides with substituted benzaldehydes: a computational and experimental study.
The Journal of organic chemistry 2007;72(11):4189-97.
2007: Paula Gomes; Nuno Vale; Rui Moreira
Cyclization-activated prodrugs.
Molecules (Basel, Switzerland) 2007;12(11):2484-506.
2007: Tânia F Oliveira; Jalmira Mulchande; Rui Moreira; Jim Iley; Margarida Archer
Crystallization and preliminary diffraction studies of porcine pancreatic elastase in complex with a novel inhibitor.
Protein and peptide letters 2007;14(1):93-5.
2007: Lina Ribeiro; Nuno Silva; Jim Iley; Jarkko Rautio; Tomi Järvinen; Helder Mota-Filipe; Rui Moreira; Eduarda Mendes
Aminocarbonyloxymethyl ester prodrugs of flufenamic acid and diclofenac: suppressing the rearrangement pathway in aqueous media.
Archiv der Pharmazie 2007;340(1):32-40.
2006: Claudia Valente; Rita C Guedes; Rui Moreira; Jim Iley; Jiri Gut; Philip J Rosenthal
Dipeptide vinyl sultams: synthesis via the Wittig-Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum.
Bioorganic & medicinal chemistry letters 2006;16(15):4115-9.
2006: Jim Iley; Rui Moreira; Luísa Martins; Rita C Guedes; Cláudio M Soares
The Bsmoc group as a novel scaffold for the design of irreversible inhibitors of cysteine proteases.
Bioorganic & medicinal chemistry letters 2006;16(10):2738-41.
2005: Rui Moreira; Ana Bela Santana; Jim Iley; João Neres; Kenneth T Douglas; Peter N Horton; Michael B Hursthouse
Design, synthesis, and enzymatic evaluation of N1-acyloxyalkyl- and N1-oxazolidin-2,4-dion-5-yl-substituted beta-lactams as novel inhibitors of human leukocyte elastase.
Journal of medicinal chemistry 2005;48(15):4861-70.
2005: Cledir Santos; Maria Luísa Mateus; Ana Paula dos Santos; Rui Moreira; Eliandre de Oliveira; Paula Gomes
Cyclization-activated prodrugs. Synthesis, reactivity and toxicity of dipeptide esters of paracetamol.
Bioorganic & medicinal chemistry letters 2005;15(6):1595-8.
2005: Maria João Araújo; Joana Bom; Rita Capela; Catarina Casimiro; Paula Chambel; Paula Gomes; Jim Iley; Francisca Lopes; José Morais; Rui Moreira; Eliandre de Oliveira; Virgílio E do Rosário; Nuno Vale
Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials.
Journal of medicinal chemistry 2005;48(3):888-92.
2004: Emília Valente; José Gomes; Rui Moreira; Jim Iley
Kinetics and mechanism of hydrolysis of N-acyloxymethyl derivatives of azetidin-2-one.
The Journal of organic chemistry 2004;69(10):3359-67.
2002: Eduarda Mendes; Tânia Furtado; João Neres; Jim Iley; Tomi Jarvinen; Jarkko Rautio; Rui Moreira
Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl esters as prodrugs of carboxylic acid agents.
Bioorganic & medicinal chemistry 2002;10(3):809-16.
2001: Alda Clemente; Ana Domingos; A P Grancho; Jim Iley; Rui Moreira; João Neres; Nuno Palma; A B Santana; Emília Valente
Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.
Bioorganic & medicinal chemistry letters 2001;11(8):1065-8.
2000: Jim Iley; H Barroso; Rui Moreira; F Lopes; T Calheiros
Acyloxymethyl as a drug protecting group. Part 7: Tertiary sulfonamidomethyl ester prodrugs of benzylpenicillin: chemical hydrolysis and anti-bacterial activity.
Bioorganic & medicinal chemistry 2000;8(7):1629-36.
2000: F Lopes; Rui Moreira; Jim Iley
Acyloxymethyl as a drug protecting group. Part 6: N-acyloxymethyl- and N-[(aminocarbonyloxy)methyl]sulfonamides as prodrugs of agents containing a secondary sulfonamide group.
Bioorganic & medicinal chemistry 2000;8(4):707-16.
1999: Jim Iley; Eduarda Mendes; Rui Moreira; S Souza
Cleavage of tertiary amidomethyl ester prodrugs of carboxylic acids by rat liver homogenates.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 1999;9(2):201-5.
1999: Luis Constantino; Paulo Paixao; Rui Moreira; M J Portela; V E Do Rosario; Jim Iley
Metabolism of primaquine by liver homogenate fractions. Evidence for monoamine oxidase and cytochrome P450 involvement in the oxidative deamination of primaquine to carboxyprimaquine.
Experimental and toxicologic pathology : official journal of the Gesellschaft für Toxikologische Pathologie 1999;51(4-5):299-303.
1999: M J Portela; Rui Moreira; Emília Valente; Luis Constantino; Jim Iley; Joao Pinto; R Rosa; Pedro Cravo; Virgílio E do Rosário
Dipeptide derivatives of primaquine as transmission-blocking antimalarials: effect of aliphatic side-chain acylation on the gametocytocidal activity and on the formation of carboxyprimaquine in rat liver homogenates.
Pharmaceutical research 1999;16(6):949-55.
1998: Jim Iley; T Calheiros; Rui Moreira
Phthalimidomethyl as a drug pro-moiety. Probing its reactivity.
Bioorganic & medicinal chemistry letters 1998;8(8):955-8.
1997: Jim Iley; Rui Moreira; T Calheiros; Eduarda Mendes
Acyloxymethyl as a drug protecting group: Part 4. The hydrolysis of tertiary amidomethyl ester prodrugs of carboxylic acid agents.
Pharmaceutical research 1997;14(11):1634-9.
1996: Rui Moreira; T Calheiros; José Cabrita; Eduarda Mendes; M Pimentel; Jim Iley
Acyloxymethyl as a drug protecting group. Part 3. Tertiary O-amidomethyl esters of penicillin G: chemical hydrolysis and anti-bacterial activity.
Pharmaceutical research 1996;13(1):70-5.