3-[4′-bromo-(1,1′-biphenyl)-4-y1]-n,n-dimethyl-3- (2-thienyl)-2-propen-1-amine: Synthesis, Cytotoxicity, And Leishmanicidal, Trypanocidal And Antimycobacterial Activities

dc.creatorDe Souza A.O.
dc.creatorHemerly F.P.
dc.creatorBusollo A.C.
dc.creatorMelo P.S.
dc.creatorMachado G.M.C.
dc.creatorMiranda C.C.
dc.creatorSanta-Rita R.M.
dc.creatorHaun M.
dc.creatorLeon L.L.
dc.creatorSato D.N.
dc.creatorDe Castro S.L.
dc.creatorDuran N.
dc.date2002
dc.date2015-06-30T16:41:24Z
dc.date2015-11-26T15:31:54Z
dc.date2015-06-30T16:41:24Z
dc.date2015-11-26T15:31:54Z
dc.date.accessioned2018-03-28T22:40:21Z
dc.date.available2018-03-28T22:40:21Z
dc.identifier
dc.identifierJournal Of Antimicrobial Chemotherapy. , v. 50, n. 5, p. 629 - 637, 2002.
dc.identifier3057453
dc.identifier
dc.identifierhttp://www.scopus.com/inward/record.url?eid=2-s2.0-0036849223&partnerID=40&md5=e5e62ea397201ea0411e5a15fa6a043a
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/101575
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/101575
dc.identifier2-s2.0-0036849223
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1262346
dc.descriptionCurrent therapies for Chagas' disease, leishmaniasis and tuberculosis are unsatisfactory because of the failure rates, significant toxicity and/or drug resistance. In this study, the compound 3-[4′-bromo- (1,1′-biphenyl)- 4-yl] -N,N-dimethyl-3- (2-thienyl) -2-propen-1-amine (IV) was synthesized and its trypanocidal, leishmanicidal and antimycobacterial activities were investigated. The cytotoxicity was determined on V79 cells with three endpoints: nucleic acid content, 3-(4,5-dimethylthiazole- 2-yl)-2,5-diphenyl tetrazolium bromide reduction and Neutral Red uptake. This compound was active against different species of mycobacteria and different life cycle stages of Trypanosoma cruzi. In experiments with trypomastigotes performed at 4° C in the presence of blood, the activity was 8.8-fold more active than the standard drug, Crystal Violet. Higher activity was achieved against Leishmania amazonensis, with an ED50/24 h of 3.0 ± 0.3 μmol/L. The effect against trypanosomatids, which suggests high activity of compound IV against promastigotes of L. amazonensis and amastigotes of T. cruzi, stimulated further studies in vitro with amastigotes interiorized in macrophages and with in vivo models. Our results indicate that mammalian V79 cells are less susceptible to the action of compound IV than promastigotes of L. amazonensis (8.0-13.3-fold) and axenic amastigotes of T. cruzi (3.5-5.9-fold).
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dc.languageen
dc.publisher
dc.relationJournal of Antimicrobial Chemotherapy
dc.rightsfechado
dc.sourceScopus
dc.title3-[4′-bromo-(1,1′-biphenyl)-4-y1]-n,n-dimethyl-3- (2-thienyl)-2-propen-1-amine: Synthesis, Cytotoxicity, And Leishmanicidal, Trypanocidal And Antimycobacterial Activities
dc.typeArtículos de revistas


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