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Synthesis and antimicrobial activity of dipeptide esters of the anti-rectroviral drug acyclovir

2005Documento de conferência Acesso aberto
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dc.contributor.authorPereira, Cláudia S.G.P.
dc.contributor.authorSantos, Cledir
dc.contributor.authorBarreira, João C.M.
dc.contributor.authorMoreira, Rui
dc.contributor.authorFerreira, Isabel C.F.R.
dc.contributor.authorEstevinho, Leticia M.
dc.contributor.authorGomes, Paula
dc.date.accessioned2011-03-23T11:42:18Z
dc.date.available2011-03-23T11:42:18Z
dc.date.issued2005
dc.description.abstractThe derivatization of ACV with amino acids has been used for the development of ACV prodrugs. In fact, the valine derivative of ACV – valacyclovir – is a pro-drug of widespread use in herpes treatment. Mitra and co-workers have recently reported the synthesis and properties of novel dipeptide prodrugs of ACV, two of which are included in the present work (3c and 3d) [1,2]. The compounds 3a-f prepared were screened for their in vitro antimicrobial activity against Gram positive (Bacillus cereus, Bacillus subtilis) and Gram negative (Pseudomonas aeruginosa, Escherichia coli) bacteria, and also for their fungicidal activity using Candida albicans. The antimicrobial activities were evaluated by diameter measurement of haloes formed by growth inhibition caused by compounds 3 at different concentrations in DMSO [3]. Compounds 3 exhibited antimicrobial activity preferentially against Gram-positive bacteria and were all inactive against Pseudomonas aeruginosa. The minimal inhibitory concentrations (MIC) could be determined for some of the compounds in the concentration range assayed. Further dilutions are being done for MIC determination of most compounds against B. cereus and B. subtilis. The determined MIC were significantly lower than those of typical standards such as ampicilline, cloramphenicol or cyclohexamide. The parent drug, ACV, was also assayed and found to be less active than the corresponding dipeptide ester derivatives. These results suggest that compounds 3 might be activated by bacterial peptidases or actively transported through bacterial cell membrane.en
dc.identifier.citationPereira, Cláudia S.G.P., Santos, Cledir; Barreira, João C.M.; Moreira, Rui; Ferreira, Isabel C.F.R.; Estevinho, Letícia, Gomes, Paula (2005). Synthesis and antimicrobial activity of dipeptide esters of the anti-rectroviral drug acyclovir. Scientia Pharmaceutica. ISSN 0036-8709. 73:2, Sup, 1. In Abstracts of the Contributions of the Joint Meeting on Medicinal Chemistrypor
dc.identifier.issn0036-8709
dc.identifier.urihttp://hdl.handle.net/10198/3724
dc.language.isoengpor
dc.peerreviewedyespor
dc.titleSynthesis and antimicrobial activity of dipeptide esters of the anti-rectroviral drug acyclovirpor
dc.typeconference object
dspace.entity.typePublication
oaire.citation.conferencePlaceViena, Áustriapor
oaire.citation.titleSupplement 1, Scientia Pharmaceutica, 73 (2) 2005- Abstracts of the Contributions of the Joint Meeting on Medicinal Chemistrypor
person.familyNameBarreira
person.familyNameFerreira
person.familyNameEstevinho
person.givenNameJoão C.M.
person.givenNameIsabel C.F.R.
person.givenNameLetícia M.
person.identifier144781
person.identifier.ciencia-id9418-CF95-9919
person.identifier.ciencia-idBA14-09D6-A406
person.identifier.orcid0000-0003-1233-0990
person.identifier.orcid0000-0003-4910-4882
person.identifier.orcid0000-0002-9249-1948
person.identifier.ridD-8269-2013
person.identifier.ridE-8500-2013
person.identifier.scopus-author-id54895546900
person.identifier.scopus-author-id36868826600
person.identifier.scopus-author-id6506577664
rcaap.rightsopenAccesspor
rcaap.typeconferenceObjectpor
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relation.isAuthorOfPublicationbd0d1537-2e03-41fb-b27a-140af9c35db8
relation.isAuthorOfPublication4a1d5ba2-1854-4ca5-89a4-73f35e964df9
relation.isAuthorOfPublication.latestForDiscovery4629b12c-39b0-4da8-8b8d-6efba5cf2d81

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