Academic literature on the topic 'Diamidinas'

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Journal articles on the topic "Diamidinas"

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COSTA, Jackson Maurício L. "O USO CLÍNICO DAS PENTAMIDINAS COM ESPECIAL REFERÊNCIA NAS LEISHMANIOSES." Acta Amazonica 23, no. 2-3 (1993): 163–72. http://dx.doi.org/10.1590/1809-43921993233172.

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O autor apresenta uma ampla revisão da literatura sobre as diamidinas aromáticas (Pentamidinas), dando ênfase à terapêutica das leishmanioses, considerando a possibilidade desta droga ser usada como segunda opção no tratamento das mesmas. Destaca aspectos relacionados à farmacodinâmica e efeitos adversos quando do uso clínico do referido medicamento.
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Yang, Gyongseon, Gahee Choi, and Joo Hwan No. "Antileishmanial Mechanism of Diamidines Involves Targeting Kinetoplasts." Antimicrobial Agents and Chemotherapy 60, no. 11 (2016): 6828–36. http://dx.doi.org/10.1128/aac.01129-16.

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ABSTRACTLeishmaniasis is a disease caused by pathogenicLeishmaniaparasites; current treatments are toxic and expensive, and drug resistance has emerged. While pentamidine, a diamidine-type compound, is one of the treatments, its antileishmanial mechanism of action has not been investigated in depth. Here we tested several diamidines, including pentamidine and its analog DB75, againstLeishmania donovaniand elucidated their antileishmanial mechanisms. We identified three promising new antileishmanial diamidine compounds with 50% effective concentrations (EC50s) of 3.2, 3.4, and 4.5 μM, while pen
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Yang, Sihyung, Tanja Wenzler, Patrik N. Miller, et al. "Pharmacokinetic Comparison To Determine the Mechanisms Underlying the Differential Efficacies of Cationic Diamidines against First- and Second-Stage Human African Trypanosomiasis." Antimicrobial Agents and Chemotherapy 58, no. 7 (2014): 4064–74. http://dx.doi.org/10.1128/aac.02605-14.

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ABSTRACTHuman African trypanosomiasis (HAT), a neglected tropical disease, is fatal without treatment. Pentamidine, a cationic diamidine, has been used to treat first-stage (hemolymphatic) HAT since the 1940s, but it is ineffective against second-stage (meningoencephalitic, or central nervous system [CNS]) infection. Novel diamidines (DB75, DB820, and DB829) have shown promising efficacy in both mouse and monkey models of first-stage HAT. However, only DB829 cured animals with second-stage infection. In this study, we aimed to determine the mechanisms underlying the differential efficacies of
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da Silva, Cristiane França, Marcos Meuser Batista, Denise da Gama Jaen Batista, et al. "In Vitro and In Vivo Studies of the Trypanocidal Activity of a Diarylthiophene Diamidine against Trypanosoma cruzi." Antimicrobial Agents and Chemotherapy 52, no. 9 (2008): 3307–14. http://dx.doi.org/10.1128/aac.00038-08.

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ABSTRACT Aromatic diamidines are DNA minor groove-binding ligands that display excellent antimicrobial activity against fungi, bacteria, and protozoa. Due to the currently unsatisfactory chemotherapy for Chagas’ disease and in view of our previous reports regarding the effect of diamidines and analogues against both in vitro and in vivo Trypanosoma cruzi infection, this study evaluated the effects of a diarylthiophene diamidine (DB1362) against both amastigotes and bloodstream trypomastigotes of T. cruzi, the etiological agent of Chagas’ disease. The data show the potent in vitro activity of D
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Nehrbass-Stuedli, Angela, David Boykin, Richard R. Tidwell, and Reto Brun. "Novel Diamidines with Activity against Babesia divergensIn Vitroand Babesia microtiIn Vivo." Antimicrobial Agents and Chemotherapy 55, no. 7 (2011): 3439–45. http://dx.doi.org/10.1128/aac.01482-10.

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ABSTRACTDicationic diamidines, such as diminazene and pentamidine, are well-studied chemotherapeutic agents with significant activity against parasitic diseases. Thein vitroactivities of novel diamidine compounds against theBabesia divergensstrains 1903B and 4201 were investigated. The most potent compound, a diphenyl furan, had a 50% inhibitory concentration (IC50) of 1.5 ng/ml. In a murine model, several test compounds were effective enough to cure mice infected withBabesia microtiat a dose of 12.5 and/or 25 mg/kg of body weight given by the subcutaneous route for 4 days. The best antibabesi
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Hall, James Edwin, John E. Kerrigan, Kishore Ramachandran, et al. "Anti-Pneumocystis Activities of Aromatic Diamidoxime Prodrugs." Antimicrobial Agents and Chemotherapy 42, no. 3 (1998): 666–74. http://dx.doi.org/10.1128/aac.42.3.666.

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ABSTRACT Aromatic dicationic compounds, such as pentamidine, have potent antimicrobial activities. Clinical use of these compounds has been restricted, however, by their toxicity and limited oral activity. A novel approach, using amidoxime derivatives as prodrugs, has recently been proposed to overcome these limitations. Although results were presented for amidoxime derivatives of only one diamidine, pentamidine, the authors in the original proposal claimed that amidoxime derivatives would work as effective prodrugs for all pharmacologically active diamidines. Nine novel amidoxime derivatives
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Lanteri, Charlotte A., Bernard L. Trumpower, Richard R. Tidwell, and Steven R. Meshnick. "DB75, a Novel Trypanocidal Agent, Disrupts Mitochondrial Function in Saccharomyces cerevisiae." Antimicrobial Agents and Chemotherapy 48, no. 10 (2004): 3968–74. http://dx.doi.org/10.1128/aac.48.10.3968-3974.2004.

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ABSTRACT The aromatic diamidines represent a class of compounds with broad-spectrum antimicrobial activity; however, their development is hindered by a lack of understanding of their mechanism of antimicrobial action. DB75 [2,5-bis(4-amidinophenyl)furan] is a trypanocidal aromatic diamidine that was originally developed as a structural analogue of the antitrypanosomal agent pentamidine. DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria. The purpose of this stu
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Mathis, Amanda M., Jacqueline L. Holman, Lisa M. Sturk, et al. "Accumulation and Intracellular Distribution of Antitrypanosomal Diamidine Compounds DB75 and DB820 in African Trypanosomes." Antimicrobial Agents and Chemotherapy 50, no. 6 (2006): 2185–91. http://dx.doi.org/10.1128/aac.00192-06.

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ABSTRACT The aromatic diamidine pentamidine has long been used to treat early-stage human African trypanosomiasis (HAT). Two analogs of pentamidine, DB75 and DB820, have been shown to be more potent and less toxic than pentamidine in murine models of trypanosomiasis. The diphenyl furan diamidine, DB75, is the active metabolite of the prodrug DB289, which is currently in phase III clinical trials as a new orally active candidate drug to treat first-stage HAT. The new aza analog, DB820, is the active diamidine of the prodrug DB844, currently undergoing preclinical evaluation as a new candidate t
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Wenzler, Tanja, David W. Boykin, Mohamed A. Ismail, James Edwin Hall, Richard R. Tidwell, and Reto Brun. "New Treatment Option for Second-Stage African Sleeping Sickness: In Vitro and In Vivo Efficacy of Aza Analogs of DB289." Antimicrobial Agents and Chemotherapy 53, no. 10 (2009): 4185–92. http://dx.doi.org/10.1128/aac.00225-09.

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ABSTRACT African sleeping sickness is a fatal parasitic disease, and all drugs currently in use for treatment have strong liabilities. It is essential to find new, effective, and less toxic drugs, ideally with oral application, to control the disease. In this study, the aromatic diamidine DB75 (furamidine) and two aza analogs, DB820 and DB829 (CPD-0801), as well as their methoxyamidine prodrugs and amidoxime metabolites, were evaluated against African trypanosomes. The active parent diamidines showed similar in vitro profiles against different Trypanosoma brucei strains, melarsoprol- and penta
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Wenzler, Tanja, Sihyung Yang, Donald A. Patrick, et al. "In VitroandIn VivoEvaluation of 28DAP010, a Novel Diamidine for Treatment of Second-Stage African Sleeping Sickness." Antimicrobial Agents and Chemotherapy 58, no. 8 (2014): 4452–63. http://dx.doi.org/10.1128/aac.02309-13.

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ABSTRACTAfrican sleeping sickness is a neglected tropical disease transmitted by tsetse flies. New and better drugs are still needed especially for its second stage, which is fatal if untreated. 28DAP010, a dipyridylbenzene analogue of DB829, is the second simple diamidine found to cure mice with central nervous system infections by a parenteral route of administration. 28DAP010 showed efficacy similar to that of DB829 in dose-response studies in mouse models of first- and second-stage African sleeping sickness. Thein vitrotime to kill, determined by microcalorimetry, and the parasite clearanc
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Dissertations / Theses on the topic "Diamidinas"

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Oliveira, Camila Belmonte. "Aceturato de diminazeno lipossomal no tratamento da infecção porTrypanosoma evansi: testes in vitro e in vivo." Universidade Federal de Santa Maria, 2014. http://repositorio.ufsm.br/handle/1/4099.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>The aim of this study was to develop and to evaluate the therapeutic efficacy of liposomes diminazene aceturate and in vitro and by using mice experimentally infected with Trypanosoma evansi. In vitro tests were performed in culture medium at concentrations of 0.25, 0.5, 1, 2 and 3 mg/ml of diminazene aceturate convetional (CDMZ) and liposomal (L-DMZ). A total of 114 rats (Rattus norvegicus) were used of in vivo test. These rats were divided into 6 groups (A, B, C, D, E and F). Group A served as a negative control (uninfected and u
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Daliry, Anissa. "Atividade, seletividade e mecanismos de ação de diamidinas aromáticas e análogos sobre Trypanosoma cruzi: um enfoque sobre o kDNA." reponame:Repositório Institucional da FIOCRUZ, 2011. https://www.arca.fiocruz.br/handle/icict/5688.

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Submitted by Anderson Silva (avargas@icict.fiocruz.br) on 2012-10-18T20:17:52Z No. of bitstreams: 1 anissa_daliry_ioc_bcm_0031_2011.pdf: 14613668 bytes, checksum: 93e5077e14be3ffeb54129fc214799c9 (MD5)<br>Made available in DSpace on 2012-10-18T20:17:52Z (GMT). No. of bitstreams: 1 anissa_daliry_ioc_bcm_0031_2011.pdf: 14613668 bytes, checksum: 93e5077e14be3ffeb54129fc214799c9 (MD5) Previous issue date: 2011<br>Universidade Federal do Rio de Janeiro. Instituto de Biofísica Carlos Chagas Filho. Rio de Janeiro, RJ, Brasil<br>A doença de Chagas, causada pelo Trypanosoma cruzi, é endêmica na
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Batista, Denise da Gama Jaén. "Estudos in vitro e in vivo da atividade biológica de fluorquinolonas, tiossemicarbazonas, diamidinas aromáticas e aromáticas e as sobre Trypanosoma cruzi." reponame:Repositório Institucional da FIOCRUZ, 2009. https://www.arca.fiocruz.br/handle/icict/4142.

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Submitted by Tatiana Oliveira (tsilva@icict.fiocruz.br) on 2012-06-06T15:32:21Z No. of bitstreams: 1 denise_gj_batista_ioc_bp_0023_2009.pdf: 5405466 bytes, checksum: 0bb4fce7e31b0593bb33cff01fa3e688 (MD5)<br>Made available in DSpace on 2012-06-06T15:32:21Z (GMT). No. of bitstreams: 1 denise_gj_batista_ioc_bp_0023_2009.pdf: 5405466 bytes, checksum: 0bb4fce7e31b0593bb33cff01fa3e688 (MD5) Previous issue date: 2009<br>Fundação Oswaldo Cruz.Instituto Oswaldo Cruz. Rio de janeiro, RJ, Brasil<br>No centenario da descoberta da doenca de Chagas (DC), esta parasitose negligenciada causada pelo Try
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Brown, Barber Jennifer Crystal. "Synthesis of Fused Heterocyclic Diamidines for the Treatment of Human African Trypanosomiasis and Fluorescence Studies of Selected Diamidines." Digital Archive @ GSU, 2010. http://digitalarchive.gsu.edu/chemistry_diss/38.

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A class of linear diamidines was synthesized for the evaluation as a treatment of Human African Trypanosomiasis. These fused heterocyclic compounds are thiazole[5,4-d]thiazoles and are of interest because the parent compound, 2,5-Bis(4-amidinophenyl)-thiazolo[5,4-d]thiazole HCl salt, which is also called DB 1929, has exhibited a low nanomolar IC50 value against Trypanosoma brucei rhodesiense and has shown selectivity for binding to the human telomere G-quadruplex over that of DNA duplex. A fluoro and a methoxy derivative have been synthesized and are currently undergoing testing for activity a
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Atsriku, Christian. "Analytical and metabolic studies of the trypanocidal diamidines." Thesis, University of Strathclyde, 2002. http://oleg.lib.strath.ac.uk:80/R/?func=dbin-jump-full&object_id=21198.

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Following the expiry of patent protection of the innovator product Berenil®, there has been an influx of substandard generic substitutes of the veterinary trypanocide in international commerce, which have been implicated as being a major contributor to the emergence of drug resistance. This situation has necessitated the development of analytical techniques, which would help safeguard the quality and efficacy of generic formulations of diminazene. A selective, accurate, precise and simple reverse-phase isocratic HPLC method for the simultaneous assay of diminazene aceturate and antipyrine (exc
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Al-Mohammadi, Abdul-Raouf A. "The diamidines as antimalarials : determinant of drugs activity." Thesis, University of Liverpool, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.414805.

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Teka, Ibrahim. "Diamidine transporters of Trypanosoma brucei." Thesis, University of Glasgow, 2011. http://theses.gla.ac.uk/2640/.

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Human African trypanosomiasis (HAT), a lethal disease caused by infection with Trypanosoma brucei rhodesiense or Trypanosoma brucei gambiense, affects a significant number of people in sub-Saharan Africa. Related trypanosome species are also responsible for veterinary trypanosomiasis in many species of domestic and wild animals, causing disruption to agricultural and economic development in one of the world’s poorest areas. Current control and management of the disease mainly relies on a handful of trypanocides that have been in use for over 50 years. The treatment is associated with numerous
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Mathis, Amanda Marie Hall James E. "Accumulation and intracellular distribution of aromatic diamidines in African trypanosomes." Chapel Hill, N.C. : University of North Carolina at Chapel Hill, 2007. http://dc.lib.unc.edu/u?/etd,985.

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Thesis (Ph. D.)--University of North Carolina at Chapel Hill, 2007.<br>Title from electronic title page (viewed Dec. 18, 2007). "... in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the School of Pharmacy." Discipline: Pharmacy; Department/School: Pharmacy.
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Hungeling, Helen [Verfasser]. "Neue Prodrugs von Diamidinen zur Therapie protozoischer Erkrankungen / Helen Hungeling." Kiel : Universitätsbibliothek Kiel, 2009. http://d-nb.info/1019869879/34.

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Tevis, Denise Susanne. "Heterocyclic Diamidines Induce Sequence Dependent Topological Changes in DNA; A Study Using Gel Electrophoresis." unrestricted, 2009. http://etd.gsu.edu/theses/available/etd-04162009-154105/.

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Thesis (M.S.)--Georgia State University, 2009.<br>Title from file title page. W. David Wilson, committee chair; Stewart A. Allison, Kathryn B. Grant, committee members. College of Arts and Sciences.Description based on contents viewed July 22, 2009. Includes bibliographical references (p. 85-87).
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Book chapters on the topic "Diamidinas"

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Mehlhorn, Heinz. "Diamidines." In Encyclopedia of Parasitology. Springer Berlin Heidelberg, 2016. http://dx.doi.org/10.1007/978-3-662-43978-4_4600.

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Mehlhorn, Heinz. "Diamidines." In Encyclopedia of Parasitology. Springer Berlin Heidelberg, 2015. http://dx.doi.org/10.1007/978-3-642-27769-6_4600-1.

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Mehlhorn, Heinz. "Aromatic Diamidines." In Encyclopedia of Parasitology. Springer Berlin Heidelberg, 2016. http://dx.doi.org/10.1007/978-3-662-43978-4_267.

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Mehlhorn, Heinz. "Aromatic Diamidines." In Encyclopedia of Parasitology. Springer Berlin Heidelberg, 2016. http://dx.doi.org/10.1007/978-3-642-27769-6_267-2.

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Negro, A., and B. Rabanal. "Aromatic Diamidines." In Encyclopedia of Chromatography, Third Edition (Print Version). CRC Press, 2009. http://dx.doi.org/10.1201/noe1420084597.ch26.

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Negro, A., and B. Rabanal. "Aromatic Diamidines." In Encyclopedia of Chromatography, Second Edition. CRC Press, 2005. http://dx.doi.org/10.1201/noe0824727857.ch26.

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"4,6-Diamidino-2-phenylindole dihydrochloride (DAPI)." In Handbook of Fluorescent Dyes and Probes. John Wiley & Sons, Inc, 2015. http://dx.doi.org/10.1002/9781119007104.ch55.

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Negro, A., and B. Rabanal. "Aromatic Diamidines: Comparison of Electrophoresis and HPLC for Analysis." In Encyclopedia of Chromatography. CRC Press, 2005. http://dx.doi.org/10.1201/noe0824727857-26.

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Conference papers on the topic "Diamidinas"

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Aten, Quentin T., Brian D. Jensen, and Sandra H. Burnett. "Testing of a Pumpless MEMS Microinjection Needle Employing Electrostatic Attraction and Repulsion of DNA." In ASME 2008 International Design Engineering Technical Conferences and Computers and Information in Engineering Conference. ASMEDC, 2008. http://dx.doi.org/10.1115/detc2008-49548.

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The ultimate goal of this work is to develop an automated MEMS-based lab-on-a-chip microinjector. This paper outlines one phase of that work: testing the feasibility of a pumpless, polysilicon MEMS microneedle for use in the proposed MEMS-based lab-on-a-chip microinjector. The pumpless MEMS microneedle operates on the principle of attraction and repulsion of DNA using electrostatic charges. Prototype microneedles were fabricated using a multi-layer surface micromachining process. DNA stained with a fluorescent dye (4‘, 6-DIAMIDINO-2-PHENYLINDOLE DIHYDROCHLORIDE or DAPI) was visualized using fl
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Tu, Shu-I., Joseph Uknalis, Deidre Patterson, and Andrew G. Gehring. "Detection of immunomagnetically captured 4',6-diamidino-2-phenyl-indole (DAPI)-labeled Escherichia coli 0157:H7 by fluorescent microscopic imaging." In Photonics East (ISAM, VVDC, IEMB), edited by Yud-Ren Chen. SPIE, 1999. http://dx.doi.org/10.1117/12.335780.

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