Literature DB >> 25576738

Antileishmanial activity of quinazoline derivatives: synthesis, docking screens, molecular dynamic simulations and electrochemical studies.

Cesar Mendoza-Martínez1, Norma Galindo-Sevilla2, José Correa-Basurto3, Victor Manuel Ugalde-Saldivar4, Rosa Georgina Rodríguez-Delgado5, Jessica Hernández-Pineda2, Cecilia Padierna-Mota6, Marcos Flores-Alamo5, Francisco Hernández-Luis7.   

Abstract

A series of quinazoline-2,4,6-triamine were synthesized and evaluated in vitro against Leishmania mexicana. Among them, N(6)-(ferrocenmethyl)quinazolin-2,4,6-triamine (H2) showed activity on promastigotes and intracellular amastigotes, as well as low cytotoxicity in mammalian cells. Docking and electrochemical studies showed the importance of both the ferrocene and the heterocyclic nucleus to the observed activity. H2 is readily oxidized electrochemically, indicating that the mechanism of action probably involves redox reactions.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antiprotozoan activity; Leishmania mexicana; Quinazoline

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Substances：

Year:  2014        PMID： 25576738     DOI： 10.1016/j.ejmech.2014.12.051

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  3 in total

1.  Identification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: synthesis and biological evaluation studies.

Authors:  Anjila Kumari; Tara Jaiswal; Vinay Kumar; Neha Hura; Gulshan Kumar; Neerupudi Kishore Babu; Ayan Acharya; Pradyot K Roy; Sankar K Guchhait; Sushma Singh
Journal:  RSC Med Chem       Date:  2022-01-06

2.  α-Mangostin Extraction from the Native Mangosteen (Garcinia mangostana L.) and the Binding Mechanisms of α-Mangostin to HSA or TRF.

Authors:  Ming Guo; Xiaomeng Wang; Xiaowang Lu; Hongzheng Wang; Peter E Brodelius
Journal:  PLoS One       Date:  2016-09-01       Impact factor: 3.240

3.  New pyrazolylpyrazoline derivatives as dual acting antimalarial-antileishamanial agents: synthesis, biological evaluation and molecular modelling simulations.

Authors:  Adnan A Bekhit; Eskedar T Lodebo; Ariaya Hymete; Hanan M Ragab; Salma A Bekhit; Kikuko Amagase; Afnan Batubara; Mohammed A S Abourehab; Alaa El-Din A Bekhit; Tamer M Ibrahim
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756
  3 in total

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