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Prevalencia de la enfermedad renal crónica y factores asociados en la población asistida en atención primaria de España: resultados del estudio IBERICAN

Llisterri, José Luis ; Micó-Pérez, Rafael Manuel ; Velilla-Zancada, Sonsoles ; [et al.]

Elsevier BV ; 2021

In: Medicina Clínica Vol. 156, No. 4 ( 2021-02), p. 157-165

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In: Medicina Clínica, Elsevier BV, Vol. 156, No. 4 ( 2021-02), p. 157-165

Type of Medium: Online Resource

ISSN: 0025-7753

URL: Article

DOI: 10.1016/j.medcli.2020.03.005

Language: Spanish

Publisher: Elsevier BV

Publication Date: 2021

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Exploring the SAR of the Ketoacyl-ACP Synthase Inhibitor GSK3011724A and Optimization around a Genotoxic Metabolite

Cunningham, Fraser ; Esquivias, Jorge ; Fernández-Menéndez, Raquel ; [et al.]

American Chemical Society (ACS) ; 2020

In: ACS Infectious Diseases Vol. 6, No. 5 ( 2020-05-08), p. 1098-1109

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In: ACS Infectious Diseases, American Chemical Society (ACS), Vol. 6, No. 5 ( 2020-05-08), p. 1098-1109

Type of Medium: Online Resource

ISSN: 2373-8227 , 2373-8227

URL: Article

DOI: 10.1021/acsinfecdis.9b00493

DOI: 10.1021/acsinfecdis.9b00493.s001

Language: English

Publisher: American Chemical Society (ACS)

Publication Date: 2020

detail.hit.zdb_id: 2806068-4

SSG: 15,3

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Tetrahydro-2-naphthyl and 2Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity

Kokkonda, Sreekanth ; Deng, Xiaoyi ; White, Karen L. ; [et al.]

American Chemical Society (ACS) ; 2016

In: Journal of Medicinal Chemistry Vol. 59, No. 11 ( 2016-06-09), p. 5416-5431

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In: Journal of Medicinal Chemistry, American Chemical Society (ACS), Vol. 59, No. 11 ( 2016-06-09), p. 5416-5431

Type of Medium: Online Resource

ISSN: 0022-2623 , 1520-4804

URL: Article

DOI: 10.1021/acs.jmedchem.6b00275

DOI: 10.1021/acs.jmedchem.6b00275.s001

DOI: 10.1021/acs.jmedchem.6b00275.s002

Language: English

Publisher: American Chemical Society (ACS)

Publication Date: 2016

detail.hit.zdb_id: 1491411-6

SSG: 15,3

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Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria

Kokkonda, Sreekanth ; Deng, Xiaoyi ; White, Karen L. ; [et al.]

American Chemical Society (ACS) ; 2020

In: Journal of Medicinal Chemistry Vol. 63, No. 9 ( 2020-05-14), p. 4929-4956

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In: Journal of Medicinal Chemistry, American Chemical Society (ACS), Vol. 63, No. 9 ( 2020-05-14), p. 4929-4956

Type of Medium: Online Resource

ISSN: 0022-2623 , 1520-4804

URL: Article

DOI: 10.1021/acs.jmedchem.0c00311

DOI: 10.1021/acs.jmedchem.0c00311.s001

DOI: 10.1021/acs.jmedchem.0c00311.s002

DOI: 10.1021/acs.jmedchem.0c00311.s003

Language: English

Publisher: American Chemical Society (ACS)

Publication Date: 2020

detail.hit.zdb_id: 1491411-6

SSG: 15,3

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Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti‐malaria Activity in Humanized Mice

Zhan, Wenhu ; Zhang, Hao ; Ginn, John ; [et al.]

Wiley ; 2021

In: Angewandte Chemie International Edition Vol. 60, No. 17 ( 2021-04-19), p. 9279-9283

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In: Angewandte Chemie International Edition, Wiley, Vol. 60, No. 17 ( 2021-04-19), p. 9279-9283

Abstract: Plasmodium falciparum proteasome (Pf20S) inhibitors are active against Plasmodium at multiple stages—erythrocytic, gametocyte, liver, and gamete activation stages—indicating that selective Pf20S inhibitors possess the potential to be therapeutic, prophylactic, and transmission‐blocking antimalarials. Starting from a reported compound, we developed a noncovalent, macrocyclic peptide inhibitor of the malarial proteasome with high species selectivity and improved pharmacokinetic properties. The compound demonstrates specific, time‐dependent inhibition of the β5 subunit of the Pf20S , kills artemisinin‐sensitive and artemisinin‐resistant P. falciparum isolates in vitro and reduces parasitemia in humanized, P. falciparum ‐infected mice.

Type of Medium: Online Resource

ISSN: 1433-7851 , 1521-3773

URL: Issue

URL: Article

DOI: 10.1002/anie.v60.17

DOI: 10.1002/anie.202015845

RVK:

VA 2100

Language: English

Publisher: Wiley

Publication Date: 2021

detail.hit.zdb_id: 2011836-3

detail.hit.zdb_id: 123227-7

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A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance

O’Neill, Paul M. ; Amewu, Richard K. ; Charman, Susan A. ; [et al.]

Springer Science and Business Media LLC ; 2017

In: Nature Communications Vol. 8, No. 1 ( 2017-05-24)

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In: Nature Communications, Springer Science and Business Media LLC, Vol. 8, No. 1 ( 2017-05-24)

Abstract: K13 gene mutations are a primary marker of artemisinin resistance in Plasmodium falciparum malaria that threatens the long-term clinical utility of artemisinin-based combination therapies, the cornerstone of modern day malaria treatment. Here we describe a multinational drug discovery programme that has delivered a synthetic tetraoxane-based molecule, E209, which meets key requirements of the Medicines for Malaria Venture drug candidate profiles. E209 has potent nanomolar inhibitory activity against multiple strains of P. falciparum and P. vivax in vitro , is efficacious against P. falciparum in in vivo rodent models, produces parasite reduction ratios equivalent to dihydroartemisinin and has pharmacokinetic and pharmacodynamic characteristics compatible with a single-dose cure. In vitro studies with transgenic parasites expressing variant forms of K13 show no cross-resistance with the C580Y mutation, the primary variant observed in Southeast Asia. E209 is a superior next generation endoperoxide with combined pharmacokinetic and pharmacodynamic features that overcome the liabilities of artemisinin derivatives.

Type of Medium: Online Resource

ISSN: 2041-1723

URL: Article

DOI: 10.1038/ncomms15159

Language: English

Publisher: Springer Science and Business Media LLC

Publication Date: 2017

detail.hit.zdb_id: 2553671-0

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Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti‐malaria Activity in Humanized Mice

Zhan, Wenhu ; Zhang, Hao ; Ginn, John ; [et al.]

Wiley ; 2021

In: Angewandte Chemie Vol. 133, No. 17 ( 2021-04-19), p. 9365-9369

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In: Angewandte Chemie, Wiley, Vol. 133, No. 17 ( 2021-04-19), p. 9365-9369

Type of Medium: Online Resource

ISSN: 0044-8249 , 1521-3757

URL: Issue

URL: Article

DOI: 10.1002/ange.v133.17

DOI: 10.1002/ange.202015845

RVK:

VA 2100

RVK:

VN 5020

Language: English

Publisher: Wiley

Publication Date: 2021

detail.hit.zdb_id: 505868-5

detail.hit.zdb_id: 506609-8

detail.hit.zdb_id: 514305-6

detail.hit.zdb_id: 505872-7

detail.hit.zdb_id: 1479266-7

detail.hit.zdb_id: 505867-3

detail.hit.zdb_id: 506259-7

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Design, synthesis and structure-activity relationship study of wollamide B; a new potential anti TB agent

Asfaw, Henok ; Laqua, Katja ; Walkowska, Anna Maria ; [et al.]

Public Library of Science (PLoS) ; 2017

In: PLOS ONE Vol. 12, No. 4 ( 2017-4-19), p. e0176088-

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In: PLOS ONE, Public Library of Science (PLoS), Vol. 12, No. 4 ( 2017-4-19), p. e0176088-

Type of Medium: Online Resource

ISSN: 1932-6203

URL: Article

DOI: 10.1371/journal.pone.0176088

DOI: 10.1371/journal.pone.0176088.g001

DOI: 10.1371/journal.pone.0176088.g002

DOI: 10.1371/journal.pone.0176088.g003

DOI: 10.1371/journal.pone.0176088.g004

DOI: 10.1371/journal.pone.0176088.t001

DOI: 10.1371/journal.pone.0176088.t002

DOI: 10.1371/journal.pone.0176088.t003

DOI: 10.1371/journal.pone.0176088.t004

DOI: 10.1371/journal.pone.0176088.t005

DOI: 10.1371/journal.pone.0176088.s001

Language: English

Publisher: Public Library of Science (PLoS)

Publication Date: 2017

detail.hit.zdb_id: 2267670-3

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Identification of KasA as the cellular target of an anti-tubercular scaffold

Abrahams, Katherine A. ; Chung, Chun-wa ; Ghidelli-Disse, Sonja ; [et al.]

Springer Science and Business Media LLC ; 2016

In: Nature Communications Vol. 7, No. 1 ( 2016-09-01)

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In: Nature Communications, Springer Science and Business Media LLC, Vol. 7, No. 1 ( 2016-09-01)

Abstract: Phenotypic screens for bactericidal compounds are starting to yield promising hits against tuberculosis. In this regard, whole-genome sequencing of spontaneous resistant mutants generated against an indazole sulfonamide (GSK3011724A) identifies several specific single-nucleotide polymorphisms in the essential Mycobacterium tuberculosis β-ketoacyl synthase ( kas ) A gene. Here, this genomic-based target assignment is confirmed by biochemical assays, chemical proteomics and structural resolution of a KasA-GSK3011724A complex by X-ray crystallography. Finally, M. tuberculosis GSK3011724A-resistant mutants increase the in vitro minimum inhibitory concentration and the in vivo 99% effective dose in mice, establishing in vitro and in vivo target engagement. Surprisingly, the lack of target engagement of the related β-ketoacyl synthases (FabH and KasB) suggests a different mode of inhibition when compared with other Kas inhibitors of fatty acid biosynthesis in bacteria. These results clearly identify KasA as the biological target of GSK3011724A and validate this enzyme for further drug discovery efforts against tuberculosis.

Type of Medium: Online Resource

ISSN: 2041-1723

URL: Article

DOI: 10.1038/ncomms12581

Language: English

Publisher: Springer Science and Business Media LLC

Publication Date: 2016

detail.hit.zdb_id: 2553671-0

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Comparative study of the disposition of levofloxacin, netilmicin and cefepime in the isolated rat lung

Martínez, María Santos Martínez ; Gandarillas, Clara Isabel Colino ; Lanao, José Martínez ; [et al.]

Oxford University Press (OUP) ; 2010

In: Journal of Pharmacy and Pharmacology Vol. 57, No. 7 ( 2010-02-18), p. 861-867

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In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 57, No. 7 ( 2010-02-18), p. 861-867

Abstract: An experimental model of artificially perfused and mechanically ventilated lung has been applied to compare the kinetic behaviour of levofloxacin, cefepime and netilmicin in this body tissue. The study has been performed to explore the usefulness of the isolated lung technique in the pharmacokinetic field, particularly to study the disposition of antibiotics in pulmonary tissue. The lung was perfused with Krebs-Henseleit medium containing 3% bovine albumin at a flow rate of 5 mL min−1. It was ventilated at 60 respirations/min with a 2-mL tidal volume of air previously humidified and warmed to 37°C. The concentrations of the above antibiotics were determined by HPLC techniques and the outflow curves were analysed by stochastic, as well as by model-dependent, methods. The results show pharmacokinetic differences among these antibiotics, which are in accordance with previously reported data, levofloxacin being the drug with the highest distribution coefficient in this tissue (1.25 ± 0.14 vs 0.39 ± 0.07 and 0.41 ± 0.06 mL g−1 for netilmicin and cefepime, respectively). Accordingly, the isolated lung of the rat, under the experimental conditions used here, constitutes an alternative model to be incorporated to pharmacokinetic studies with a great potential use for those drugs that show a pharmacological or toxicological action depending on the kinetic profile in the lung tissue.

Type of Medium: Online Resource

ISSN: 0022-3573 , 2042-7158

URL: Article

DOI: 10.1211/0022357056479

Language: English

Publisher: Oxford University Press (OUP)

Publication Date: 2010

detail.hit.zdb_id: 2041988-0

detail.hit.zdb_id: 2050532-2

SSG: 15,3

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