Literature DB >> 15546709

Synthesis and antitrypanosomal profile of new functionalized 1,3,4-thiadiazole-2-arylhydrazone derivatives, designed as non-mutagenic megazol analogues.

Samir A Carvalho1, Edson F da Silva, Ricardo M Santa-Rita, Solange L de Castro, Carlos A M Fraga.   

Abstract

In this work we reported the synthesis and the trypanocidal profile of new 1,3,4-thiadiazole-2-arylhydrazone derivatives of nitroimidazole series (4) or phenyl series (5), designed by exploring the molecular hybridization approach between megazol (2) and guanyl hydrazone derivative (3). The evaluation of the activity against bloodstream trypomastigote forms of Trypanosoma cruzi forms lead us to identify a new potent trypamomicide prototype, that is, brazilizone A (4k), which present an IC50/24 h=5.3 microM.

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Year:  2004        PMID： 15546709     DOI： 10.1016/j.bmcl.2004.10.007

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  10 in total

1.  In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi.

Authors:  K Salomão; E M de Souza; S A Carvalho; E F da Silva; C A M Fraga; H S Barbosa; S L de Castro
Journal:  Antimicrob Agents Chemother       Date:  2010-03-15       Impact factor: 5.191

2.  Application of linear discriminant analysis in the virtual screening of antichagasic drugs through trypanothione reductase inhibition.

Authors:  Julián J Prieto; Alan Talevi; Luis E Bruno-Blanch
Journal:  Mol Divers       Date:  2006-09-21       Impact factor: 2.943

3.  Bis[(5-phenyl-1,3,4-thia-diazol-2-yl)sulfan-yl]methane.

Authors:  He-Wen Wang; Yan Gao; Wei Wang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-11-06

4.  5-(3-Nitro-benz-yl)-1,3,4-thia-diazol-2-amine.

Authors:  Samir A Carvalho; Larisse O de Feitosa; Edson F da Silva; Edward R T Tiekink; James L Wardell; Solange M S V Wardell
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-11-25

5.  Screening of Potential anti-Trypanosoma cruzi Candidates: In Vitro and In Vivo Studies.

Authors:  Maria de Nazaré C Soeiro; Solange Lisboa de Castro
Journal:  Open Med Chem J       Date:  2011-03-09

6.  2-(4-Methyl-phen-yl)-5-[({[5-(4-methyl-phen-yl)-1,3,4-thia-diazol-2-yl]sulfan-yl}meth-yl)sulfan-yl]-1,3,4-thia-diazole.

Authors:  Yong Wang; Wen-Ge Zhang; Yu-Bo Wang; Jing-Wen Yu; Lin Zhou
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-02-24

7.  Studies of genotoxicity and mutagenicity of nitroimidazoles: demystifying this critical relationship with the nitro group.

Authors:  Núbia Boechat; Alcione S Carvalho; Kelly Salomão; Solange L de Castro; Carlos F Araujo-Lima; Francisco V C Mello; Israel Felzenszwalb; Claudia A F Aiub; Taline Ramos Conde; Helena P S Zamith; Rolf Skupin; Günter Haufe
Journal:  Mem Inst Oswaldo Cruz       Date:  2015-05-26       Impact factor: 2.743

8.  Selective Cytotoxicity of 1,3,4-Thiadiazolium Mesoionic Derivatives on Hepatocarcinoma Cells (HepG2).

Authors:  Gustavo Jabor Gozzi; Amanda do Rocio Andrade Pires; Glaucio Valdameri; Maria Eliane Merlin Rocha; Glaucia Regina Martinez; Guilhermina Rodrigues Noleto; Alexandra Acco; Carlos Eduardo Alves de Souza; Aurea Echevarria; Camilla Moretto Dos Reis; Attilio Di Pietro; Sílvia Maria Suter Correia Cadena
Journal:  PLoS One       Date:  2015-06-17       Impact factor: 3.240

9.  Megazol and its bioisostere 4H-1,2,4-triazole: comparing the trypanocidal, cytotoxic and genotoxic activities and their in vitro and in silico interactions with the Trypanosoma brucei nitroreductase enzyme.

Authors:  Alcione Silva de Carvalho; Kelly Salomão; Solange Lisboa de Castro; Taline Ramos Conde; Helena Pereira da Silva Zamith; Ernesto Raúl Caffarena; Belinda Suzette Hall; Shane Robert Wilkinson; Núbia Boechat
Journal:  Mem Inst Oswaldo Cruz       Date:  2014-03-18       Impact factor: 2.743

10.  Antiprotozoal activity of (E)-cinnamic N-acylhydrazone derivatives.

Authors:  Samir Aquino Carvalho; Marcel Kaiser; Reto Brun; Edson Ferreira da Silva; Carlos Alberto Manssour Fraga
Journal:  Molecules       Date:  2014-12-05       Impact factor: 4.411
  10 in total

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