Literature DB >> 25147146

2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.

Marcos Veríssimo de Oliveira Cardoso1, Lucianna Rabelo Pessoa de Siqueira2, Elany Barbosa da Silva2, Lívia Bandeira Costa2, Marcelo Zaldini Hernandes2, Marcelo Montenegro Rabello2, Rafaela Salgado Ferreira3, Luana Faria da Cruz3, Diogo Rodrigo Magalhães Moreira4, Valéria Rêgo Alves Pereira5, Maria Carolina Accioly Brelaz de Castro5, Paul V Bernhardt6, Ana Cristina Lima Leite2.   

Abstract

The present work reports on the synthesis, anti-Trypanosoma cruzi activities and docking studies of a novel series of 2-(pyridin-2-yl)-1,3-thiazoles derived from 2-pyridine thiosemicarbazone. The majority of these compounds are potent cruzain inhibitors and showed excellent inhibition on the trypomastigote form of the parasite, and the resulting structure-activity relationships are discussed. Together, these data present a novel series of thiazolyl hydrazones with potential effects against Chagas disease and they could be important leads in continuing development against Chagas disease.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  2-Pyridine thiosemicarbazone; Chagas disease; Hydrazones; Thiazoles; Trypanosoma cruzi

Mesh：

Substances：

Year:  2014        PMID： 25147146     DOI： 10.1016/j.ejmech.2014.08.012

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


  7 in total

Review 1.  Thiazole Ring-A Biologically Active Scaffold.

Authors:  Anthi Petrou; Maria Fesatidou; Athina Geronikaki
Journal:  Molecules       Date:  2021-05-25       Impact factor: 4.411

2.  Crystal structure of a 1,1,2,2-tetra-chloro-ethane-solvated hydrazinecarbo-thio-amide compound.

Authors:  Sayed Riyadh; David L Hughes; Musa A Said
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2017-08-01

3.  Chitosan-MgO Nanocomposite: One Pot Preparation and Its Utility as an Ecofriendly Biocatalyst in the Synthesis of Thiazoles and [1,3,4]thiadiazoles.

Authors:  Sayed M Riyadh; Khaled D Khalil; Ateyatallah Aljuhani
Journal:  Nanomaterials (Basel)       Date:  2018-11-08       Impact factor: 5.076

4.  4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis.

Authors:  Daniela Secci; Simone Carradori; Anél Petzer; Paolo Guglielmi; Melissa D'Ascenzio; Paola Chimenti; Donatella Bagetta; Stefano Alcaro; Gokhan Zengin; Jacobus P Petzer; Francesco Ortuso
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

5.  New Hydrazinothiazole Derivatives of Usnic Acid as Potent Tdp1 Inhibitors.

Authors:  Aleksander S Filimonov; Arina A Chepanova; Olga A Luzina; Alexandra L Zakharenko; Olga D Zakharova; Ekaterina S Ilina; Nadezhda S Dyrkheeva; Maxim S Kuprushkin; Anton V Kolotaev; Derenik S Khachatryan; Jinal Patel; Ivanhoe K H Leung; Raina Chand; Daniel M Ayine-Tora; Johannes Reynisson; Konstantin P Volcho; Nariman F Salakhutdinov; Olga I Lavrik
Journal:  Molecules       Date:  2019-10-15       Impact factor: 4.411

6.  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

7.  Trypanocidal Activity of Flavanone Derivatives.

Authors:  Gabriela Maciel Diogo; Josimara Souza Andrade; Policarpo Ademar Sales Junior; Silvane Maria Fonseca Murta; Viviane Martins Rebello Dos Santos; Jason Guy Taylor
Journal:  Molecules       Date:  2020-01-17       Impact factor: 4.411
  7 in total

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