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Publikationer i urvalet

23 träffar

Bibliografisk träff 2024-05-31

Novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives and their antitrypanosomal activities against T.brucei.

Taylor AE, Hering M, Elsegood MRJ, Teat SJ, Weaver GW, Arroo RRJ, Kaiser M, Maeser P, Bhambra AS.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2024.129825

Bibliografisk träff 2023-11-20

Discovery of New Fusobacterium nucleatum Inhibitors to Attenuate Migratory Capability of Colon Cancer Cells by the Drug Repositioning Strategy.

Pan Z, Zhou C, Bai X, Wang F, Hong J, Fang JY, Huang Y, Sheng C.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c00281

Bibliografisk träff 2023-11-15

Discovery of an orally active nitrothiophene-based antitrypanosomal agent.

Ajayi O, Metibemu DS, Crown O, Adeyinka OS, Kaiser M, Shoji N, Silva M, Rodriguez A, Ogungbe IV.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2023.115954

Bibliografisk träff 2023-09-20

Synthesis and Biophysical and Biological Studies of N-Phenylbenzamide Derivatives Targeting Kinetoplastid Parasites.

Nué-Martinez JJ, Cisneros D, Moreno-Blázquez MDV, Fonseca-Berzal C, Manzano JI, Kraeutler D, Ungogo MA, Aloraini MA, Elati HAA, Ibáñez-Escribano A, Lagartera L, Herraiz T, Gamarro F, de Koning HP, Gómez-Barrio A, Dardonville C.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.3c00697

Bibliografisk träff 2023-09-18

Bis-6-amidino-benzothiazole Derivative that Cures Experimental Stage 1 African Trypanosomiasis with a Single Dose.

Racané L, Ptiček L, Kostrun S, Raić-Malić S, Taylor MC, Delves M, Alsford S, Olmo F, Francisco AF, Kelly JM.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.3c01051

Bibliografisk träff 2020-09-18

Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.

Thompson AM, O'Connor PD, Marshall AJ, Francisco AF, Kelly JM, Riley J, Read KD, Perez CJ, Cornwall S, Thompson RCA, Keenan M, White KL, Charman SA, Zulfiqar B, Sykes ML, Avery VM, Chatelain E, Denny WA.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112849

Bibliografisk träff 2020-08-04

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.

Fersing C, Boudot C, Paoli-Lombardo R, Primas N, Pinault E, Hutter S, Castera-Ducros C, Kabri Y, Pedron J, Bourgeade-Delmas S, Sournia-Saquet A, Stigliani JL, Valentin A, Azqueta A, Muruzabal D, Destere A, Wyllie S, Fairlamb AH, Corvaisier S, Since M, Malzert-Fréon A, Di Giorgio C, Rathelot P, Azas N, Courtioux B, Vanelle P, Verhaeghe P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112668

Bibliografisk träff 2020-07-08

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.

Fersing C, Boudot C, Castera-Ducros C, Pinault E, Hutter S, Paoli-Lombardo R, Primas N, Pedron J, Seguy L, Bourgeade-Delmas S, Sournia-Saquet A, Stigliani JL, Brossas JY, Paris L, Valentin A, Wyllie S, Fairlamb AH, Boutet-Robinet É, Corvaisier S, Since M, Malzert-Fréon A, Destere A, Mazier D, Rathelot P, Courtioux B, Azas N, Verhaeghe P, Vanelle P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112558

Bibliografisk träff 2020-02-06

New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.

Pedron J, Boudot C, Brossas JY, Pinault E, Bourgeade-Delmas S, Sournia-Saquet A, Boutet-Robinet E, Destere A, Tronnet A, Bergé J, Bonduelle C, Deraeve C, Pratviel G, Stigliani JL, Paris L, Mazier D, Corvaisier S, Since M, Malzert-Fréon A, Wyllie S, Milne R, Fairlamb AH, Valentin A, Courtioux B, Verhaeghe P.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.9b00566

Bibliografisk träff 2020-01-08

Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-b]pyridazines for the Treatment of Human African Trypanosomiasis.

Tear WF, Bag S, Diaz-Gonzalez R, Ceballos-Pérez G, Rojas-Barros DI, Cordon-Obras C, Pérez-Moreno G, García-Hernández R, Martinez-Martinez MS, Ruiz-Perez LM, Gamarro F, Gonzalez Pacanowska D, Caffrey CR, Ferrins L, Manzano P, Navarro M, Pollastri MP.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.9b01741

Bibliografisk träff 2019-04-06

Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.

Georgiadis MO, Kourbeli V, Ioannidou V, Karakitsios E, Papanastasiou I, Tsotinis A, Komiotis D, Vocat A, Cole ST, Taylor MC, Kelly JM.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2019.04.010

Bibliografisk träff 2018-12-19

Nongenotoxic 3-Nitroimidazo[1,2-a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity.

Fersing C, Basmaciyan L, Boudot C, Pedron J, Hutter S, Cohen A, Castera-Ducros C, Primas N, Laget M, Casanova M, Bourgeade-Delmas S, Piednoel M, Sournia-Saquet A, Belle Mbou V, Courtioux B, Boutet-Robinet É, Since M, Milne R, Wyllie S, Fairlamb AH, Valentin A, Rathelot P, Verhaeghe P, Vanelle P, Azas N.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.8b00347

Bibliografisk träff 2018-08-01

8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.

Fersing C, Boudot C, Pedron J, Hutter S, Primas N, Castera-Ducros C, Bourgeade-Delmas S, Sournia-Saquet A, Moreau A, Cohen A, Stigliani JL, Pratviel G, Crozet MD, Wyllie S, Fairlamb A, Valentin A, Rathelot P, Azas N, Courtioux B, Verhaeghe P, Vanelle P.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2018.07.064

Bibliografisk träff 2018-06-05

Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.

Pedron J, Boudot C, Hutter S, Bourgeade-Delmas S, Stigliani JL, Sournia-Saquet A, Moreau A, Boutet-Robinet E, Paloque L, Mothes E, Laget M, Vendier L, Pratviel G, Wyllie S, Fairlamb A, Azas N, Courtioux B, Valentin A, Verhaeghe P.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2018.06.001

Bibliografisk träff 2018-04-06

2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.

Giroud M, Kuhn B, Saint-Auret S, Kuratli C, Martin RE, Schuler F, Diederich F, Kaiser M, Brun R, Schirmeister T, Haap W.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.7b01870

Bibliografisk träff 2017-10-27

Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.

Thompson AM, Marshall AJ, Maes L, Yarlett N, Bacchi CJ, Gaukel E, Wring SA, Launay D, Braillard S, Chatelain E, Mowbray CE, Denny WA.

Bioorg Med Chem Lett · brief-report; research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.10.067

Bibliografisk träff 2017-05-22

Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases.

Ang CW, Jarrad AM, Cooper MA, Blaskovich MAT.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.7b00143

Bibliografisk träff 2015-03-31

Antileishmanial pharmacomodulation in 8-nitroquinolin-2(1H)-one series.

Kieffer C, Cohen A, Verhaeghe P, Paloque L, Hutter S, Castera-Ducros C, Laget M, Rault S, Valentin A, Rathelot P, Azas N, Vanelle P.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2015.03.064

Bibliografisk träff 2013-09-11

Targeting the human parasite Leishmania donovani: discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series.

Castera-Ducros C, Paloque L, Verhaeghe P, Casanova M, Cantelli C, Hutter S, Tanguy F, Laget M, Remusat V, Cohen A, Crozet MD, Rathelot P, Azas N, Vanelle P.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2013.09.002

Bibliografisk träff 2012-06-07

Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.

Arán VJ, Kaiser M, Dardonville C.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2012.06.004

Bibliografisk träff 2011-02-26

1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.

Trunz BB, Jędrysiak R, Tweats D, Brun R, Kaiser M, Suwiński J, Torreele E.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2011.01.071

Bibliografisk träff 2010-12-10

Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.

Samant BS, Sukhthankar MG.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.12.040

Bibliografisk träff 2010-05-03

Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.

Sokolova AY, Wyllie S, Patterson S, Oza SL, Read KD, Fairlamb AH.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article · DOI 10.1128/aac.00332-10

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Publikationer i urvalet

Novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives and their antitrypanosomal activities against T.brucei.

Discovery of New <i>Fusobacterium nucleatum</i> Inhibitors to Attenuate Migratory Capability of Colon Cancer Cells by the Drug Repositioning Strategy.

Discovery of an orally active nitrothiophene-based antitrypanosomal agent.

Synthesis and Biophysical and Biological Studies of <i>N</i>-Phenylbenzamide Derivatives Targeting Kinetoplastid Parasites.

Bis-6-amidino-benzothiazole Derivative that Cures Experimental Stage 1 African Trypanosomiasis with a Single Dose.

Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.

New 8-Nitroquinolinone Derivative Displaying Submicromolar <i>in Vitro</i> Activities against Both <i>Trypanosoma brucei</i> and <i>cruzi</i>.

Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-<i>b</i>]pyridazines for the Treatment of Human African Trypanosomiasis.

Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.

Nongenotoxic 3-Nitroimidazo[1,2-<i>a</i>]pyridines Are NTR1 Substrates That Display Potent <i>in Vitro</i> Antileishmanial Activity.

8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.

Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.

2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.

Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.

Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases.

Antileishmanial pharmacomodulation in 8-nitroquinolin-2(1H)-one series.

Targeting the human parasite Leishmania donovani: discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series.

Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.

1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.

Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.

Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.