Utilize este identificador para referenciar este registo:
https://hdl.handle.net/1822/72844
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Campo DC | Valor | Idioma |
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dc.contributor.author | Bacelar, Ana H. | por |
dc.contributor.author | Carvalho, M. Alice | por |
dc.contributor.author | Proença, M. Fernanda R. P. | por |
dc.date.accessioned | 2021-05-25T15:01:12Z | - |
dc.date.issued | 2010-07-01 | - |
dc.date.submitted | 2010-02 | - |
dc.identifier.citation | Bacelar, A. H., Carvalho, M. A., Proença, M. F. (2010). Synthesis and in vitro evaluation of substituted pyrimido [5, 4-d] pyrimidines as a novel class of Antimycobacterium tuberculosis agents. European journal of medicinal chemistry, 45(7), 3234-3239 | por |
dc.identifier.issn | 0223-5234 | por |
dc.identifier.uri | https://hdl.handle.net/1822/72844 | - |
dc.description.abstract | Novel pyrimido[5,4-d]pyrimidines were efficiently synthesized and evaluated for antibacterial activity against Mycobacterium tuberculosis strain H(37)Rv. This new structural class of compounds showed high activity against the bacilli. The activity depends on the substituents present in N-3 and C-8 of the pyrimido[5,4-d]pyrimidine core. Compounds having a 4-MeOC(6)H(4), a Ph or a 4-FC(6)H(4) group as the substituent on C-8 and a 4'-pyridinyl, a Ph or 2'-furyl group as the substituent on N-3 were active. The highest activity was registered for compounds having 4-FC(6)H(4) or 4-MeOC(6)H(4) as substituents in C-8 and a heteroaryl group as substituent in N-3. The new compounds showed high potency and promising antitubercular activity, as is the case of N[8-[(4-fluorophenyl)amino]-4-iminopyrimido[5,4-d]pyrimidin-3(4H)-yl]isonicotinamide with an IC(90) = 3.58 mu g/mL, and should be regarded as new hits for further development as a novel class of Antimycobacterium tuberculosis agents. (C) 2010 Elsevier Masson SAS. All rights reserved. | por |
dc.description.sponsorship | Antimycobacterial data were provided by the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) through a research and development contract with the US National Institute of Allergy and Infectious Diseases. The NMR spectrometer (Bruker 400 Avance III) is part of the National NMR Network and was purchased in the framework of the National Programme for Scientific Re-equipment, contract REDE/1517/RMN/2005, with funds from POCI 2010 (FEDER) and Fundacao para a Ciencia e a Tecnologia (FCT). The authors gratefully acknowledge the financial support by Universidade do Minho, Centro de Quimica and Fundacao para a Ciencia e a Tecnologia (project PPCDT/QUI/59356/2004 and a PhD grant awarded to Ana Bacelar SFRH/BD/24959/2005). | por |
dc.language.iso | eng | por |
dc.publisher | Elsevier 1 | por |
dc.rights | closedAccess | por |
dc.subject | Antimicrobial | por |
dc.subject | Tuberculosis | por |
dc.subject | Pyrimido[5,4-d]pyrimidine | por |
dc.subject | Antimycobacterial activity | por |
dc.title | Synthesis and in vitro evaluation of substituted pyrimido[5,4-d]pyrimidines as a novel class of Antimycobacterium tuberculosis agents | por |
dc.type | article | - |
dc.peerreviewed | yes | por |
dc.relation.publisherversion | https://www.sciencedirect.com/science/article/pii/S0223523410002618 | por |
oaire.citationStartPage | 3234 | por |
oaire.citationEndPage | 3239 | por |
oaire.citationIssue | 7 | por |
oaire.citationVolume | 45 | por |
dc.date.updated | 2021-05-21T08:34:07Z | - |
dc.identifier.doi | 10.1016/j.ejmech.2010.03.047 | por |
dc.date.embargo | 10000-01-01 | - |
dc.subject.fos | Ciências Naturais::Ciências Químicas | por |
dc.subject.wos | Science & Technology | - |
sdum.export.identifier | 10753 | - |
sdum.journal | European Journal of Medicinal Chemistry | por |
Aparece nas coleções: | CDQuim - Artigos (Papers) |
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1-s2.0-S0223523410002618-main.pdf Acesso restrito! | 257,42 kB | Adobe PDF | Ver/Abrir |