Literature DB >> 27100030

Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.

Daniela Secci1, Simone Carradori2, Bruna Bizzarri1, Paola Chimenti1, Celeste De Monte1, Adriano Mollica3, Daniela Rivanera4, Alessandra Zicari5, Emanuela Mari5, Gokhan Zengin6, Abdurrahman Aktumsek6.   

Abstract

Pursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nitrogen with differently substituted (NO2, NH2, Cl and F) benzyl groups. These compounds were tested to evaluate their minimum inhibitory concentration (MIC) against several clinical Candida spp. with respect to topical and systemic reference drugs (clotrimazole, fluconazole, ketoconazole, miconazole, tioconazole, amphotericin B). Moreover, anti-oxidant properties were also evaluated by using different protocols including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelating and phosphomolybdenum assays. Moreover, for the most active derivatives we assessed the toxicity (CC50) against Hep2 human cells in order to characterize them as multi-target agents for fungal infections.
Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anti-Candida activity; Anti-oxidant agents; Cytotoxicity; Metal chelating agents; N-benzyl-4-thiazolidinones

Mesh:

Substances:

Year:  2016        PMID: 27100030     DOI: 10.1016/j.ejmech.2016.04.012

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


  8 in total

1.  A complex game of hide and seek: the search for new antifungals.

Authors:  Huy X Ngo; Sylvie Garneau-Tsodikova; Keith D Green
Journal:  Medchemcomm       Date:  2016-05-17       Impact factor: 3.597

2.  Synthesis, characterization, biological evaluation and molecular docking studies of 2-(1H-benzo[d]imidazol-2-ylthio)-N-(substituted 4-oxothiazolidin-3-yl) acetamides.

Authors:  Snehlata Yadav; Balasubramanian Narasimhan; Siong M Lim; Kalavathy Ramasamy; Mani Vasudevan; Syed Adnan Ali Shah; Manikandan Selvaraj
Journal:  Chem Cent J       Date:  2017-12-22       Impact factor: 4.215

3.  Analysis of imidazoles and triazoles in biological samples after MicroExtraction by packed sorbent.

Authors:  Cristina Campestre; Marcello Locatelli; Paolo Guglielmi; Elisa De Luca; Giuseppe Bellagamba; Sergio Menta; Gokhan Zengin; Christian Celia; Luisa Di Marzio; Simone Carradori
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

4.  The design, synthesis, and in vitro trypanocidal and leishmanicidal activities of 1,3-thiazole and 4-thiazolidinone ester derivatives.

Authors:  Muhammad Haroon; Mabilly Cox Holanda de Barros Dias; Aline Caroline da Silva Santos; Valéria Rêgo Alves Pereira; Luiz Alberto Barros Freitas; Rodolfo Bento Balbinot; Vanessa Kaplum; Celso Vataru Nakamura; Luiz Carlos Alves; Fábio André Brayner; Ana Cristina Lima Leite; Tashfeen Akhtar
Journal:  RSC Adv       Date:  2021-01-11       Impact factor: 3.361

5.  Neem oil nanoemulsions: characterisation and antioxidant activity.

Authors:  Federica Rinaldi; Patrizia Nadia Hanieh; Catia Longhi; Simone Carradori; Daniela Secci; Gokhan Zengin; Maria Grazia Ammendolia; Elena Mattia; Elena Del Favero; Carlotta Marianecci; Maria Carafa
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

6.  Novel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group acting as human carbonic anhydrase IX inhibitors.

Authors:  Özlen Güzel-Akdemir; Andrea Angeli; Kübra Demir; Claudiu T Supuran; Atilla Akdemir
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

7.  Development of Thiazolidinones as Fungal Carbonic Anhydrase Inhibitors.

Authors:  Özlen Güzel-Akdemir; Simone Carradori; Rossella Grande; Kübra Demir-Yazıcı; Andrea Angeli; Claudiu T Supuran; Atilla Akdemir
Journal:  Int J Mol Sci       Date:  2020-04-22       Impact factor: 5.923

Review 8.  Saturated Five-Membered Thiazolidines and Their Derivatives: From Synthesis to Biological Applications.

Authors:  Nusrat Sahiba; Ayushi Sethiya; Jay Soni; Dinesh K Agarwal; Shikha Agarwal
Journal:  Top Curr Chem (Cham)       Date:  2020-03-23
  8 in total

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