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Espinosa-Buitrago, TeresaAuthor

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October 22, 2024
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3-Alkoxy-1-Benzyl-5-Nitroindazole Derivatives Are Potent Antileishmanial Compounds

Publicated to: International Journal Of Molecular Sciences. 25 (19): 10582- - 2024-10-01 25(19), DOI: 10.3390/ijms251910582

Authors:

Mollineda-Diogo, N; Sifontes-Rodríguez, S; Aguirre-García, MM; Escalona-Montaño, AR; Espinosa-Buitrago, T; Mondragon-Flores, R; Mondragón-Castelán, ME; Meneses-Marcel, A; Pérez-Olvera, O; Sánchez-Almaraz, DA; Perez-Castillo, Y; Arán-Redó, V
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Affiliations

Consejo Super Invest Cient Espana, Inst Quim Med, Juan Cierva 3, Madrid 28006, Spain - Author
Inst Politecn Nacl CINVESTAV, Ctr Invest & Estudios Avanzados, Dept Bioquim, Mexico City 14080, Mexico - Author
Univ Cent Marta Abreu de Las Villas, Ctr Bioact Quim, Santa Clara 250512, Villa Clara, Cuba - Author
Univ Las Amer, Fac Ingn & Ciencias Aplicadas, Quito 170125, Ecuador - Author
Univ Las Amer, Grp Bioquimioinformat, Quito 170125, Ecuador - Author
Univ Nacl Autonoma Mexico, Consejo Nacl Humanidades Ciencias & Tecnol CONAHCY, Inst Invest Biomed, Mexico City 14080, Mexico - Author
Univ Nacl Autonoma Mexico, Fac Med, Unidad Invest UNAM INC, Inst Nacl Cardiol Ignacio Chavez, Mexico City 14080, Mexico - Author
Univ San Pablo CEU, CEU Univ, Fac Farm, Madrid 28660, Spain - Author
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Abstract

Indazoles have previously been identified as molecules with antiprotozoal activity. In this study, we evaluate the in vitro activity of thirteen 3-alkoxy-1-benzyl-5-nitroindazole derivatives (series D) against L. amazonensis, L. infantum, and L. mexicana. In vitro, cytotoxicity against mouse peritoneal macrophages and growth inhibitory activity in promastigotes were evaluated for all compounds, and those showing adequate activity and selectivity were tested against intracellular amastigotes. Transmission and scanning electron microscopy were employed to study the effects of 3-alkoxy-1-benzyl-5-nitroindazole and 2-benzyl-5-nitroindazolin-3-one derivatives on promastigotes of L. amazonensis. Compounds NV6 and NV8 were active in the two life stages of the three species, with the latter showing the best indicators of activity and selectivity. 3-alkoxy-1-benzyl-5-nitroindazole derivatives (series D) showed in vitro activity comparable to that of amphotericin B against the promastigote stage of Leishmania spp. Two compounds were also found to be active the amastigote stage. Electron microscopy studies confirmed the antileishmanial activity of the indazole derivatives studied and support future research on this family of compounds as antileishmanial agents.
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Keywords

2-benzyl-5-nitroindazolin-3-one2h-indazoles3-alkoxy-1-benzyl-5-nitroindazole5-nitroindazoleAmastigoteAnimalsAntileishmanial activitAntileishmanial activityAntiprotozoal agentsAssaIn-vitroIndazolesLeishmaniaLeishmaniasisMacrophages, peritonealMiceMice, inbred balb cPromastigote

Quality index

Bibliometric impact. Analysis of the contribution and dissemination channel

The work has been published in the journal INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES due to its progression and the good impact it has achieved in recent years, according to the agency WoS (JCR), it has become a reference in its field. In the year of publication of the work, 2024 there are still no calculated indicators, but in 2023, it was in position 72/320, thus managing to position itself as a Q1 (Primer Cuartil), in the category Biochemistry & Molecular Biology.

Independientemente del impacto esperado determinado por el canal de difusión, es importante destacar el impacto real observado de la propia aportación.

Según las diferentes agencias de indexación, el número de citas acumuladas por esta publicación hasta la fecha 2026-02-27:

  • WoS: 4
  • Scopus: 4
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Impact and social visibility

From the perspective of influence or social adoption, and based on metrics associated with mentions and interactions provided by agencies specializing in calculating the so-called "Alternative or Social Metrics," we can highlight as of 2026-02-27:

  • The use, from an academic perspective evidenced by the Altmetric agency indicator referring to aggregations made by the personal bibliographic manager Mendeley, gives us a total of: 7.
  • The use of this contribution in bookmarks, code forks, additions to favorite lists for recurrent reading, as well as general views, indicates that someone is using the publication as a basis for their current work. This may be a notable indicator of future more formal and academic citations. This claim is supported by the result of the "Capture" indicator, which yields a total of: 7 (PlumX).

With a more dissemination-oriented intent and targeting more general audiences, we can observe other more global scores such as:

    It is essential to present evidence supporting full alignment with institutional principles and guidelines on Open Science and the Conservation and Dissemination of Intellectual Heritage. A clear example of this is:

    • The work has been submitted to a journal whose editorial policy allows open Open Access publication.
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    Leadership analysis of institutional authors

    This work has been carried out with international collaboration, specifically with researchers from: Cuba; Ecuador; Mexico.

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    Awards linked to the item

    Funding was provided in part by The International Collaboration Project Strengthening and development of research capacities for the treatment of neglected and neglected parasitic diseases, developed between the Complutense University of Madrid and the Centro de Bioactivos Quimicos of Cuba.
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