Literature DB >> 17367894

A comparative study of mesoionic compounds in Leishmania sp. and toxicity evaluation.

Raquel F Rodrigues1, Edson F da Silva, Aurea Echevarria, Renata Fajardo-Bonin, Veronica F Amaral, Leonor L Leon, Marilene M Canto-Cavalheiro.   

Abstract

In this first study, a series of mesoionic compounds like 1,3,4-thiadiazolium-2-phenylamine derivatives were synthesized and studied in Leishmania amazonensis. The cytotoxic effects of these compounds on the host cells were investigated and the antileishmanial in vitro activity was compared with other species of Leishmania (Leishmania chagasi and Leishmania braziliensis). The compounds presented lower toxicity in murine macrophages than the reference drug pentamidine. The halogen derivatives 5, 6, 8 and 13 (4-F, 4-Cl, 4-Br and 3-Cl) were the most active compounds among all the species tested.

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Year:  2007        PMID: 17367894     DOI: 10.1016/j.ejmech.2006.12.026

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


  5 in total

Review 1.  Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.

Authors:  Advait S Nagle; Shilpi Khare; Arun Babu Kumar; Frantisek Supek; Andriy Buchynskyy; Casey J N Mathison; Naveen Kumar Chennamaneni; Nagendar Pendem; Frederick S Buckner; Michael H Gelb; Valentina Molteni
Journal:  Chem Rev       Date:  2014-11-03       Impact factor: 60.622

2.  Antileishmanial activity of 1,3,4-thiadiazolium-2-aminide in mice infected with Leishmania amazonensis.

Authors:  Raquel F Rodrigues; Karen S Charret; Edson F da Silva; Aurea Echevarria; Verônica F Amaral; Leonor L Leon; Marilene M Canto-Cavalheiro
Journal:  Antimicrob Agents Chemother       Date:  2008-11-17       Impact factor: 5.191

3.  Derivatives of the triaminoguanidinium ion, 5. Acylation of triaminoguanidines leading to symmetrical tris(acylamino)guanidines and mesoionic 1,2,4-triazolium-3-aminides.

Authors:  Jan Szabo; Julian Greiner; Gerhard Maas
Journal:  Beilstein J Org Chem       Date:  2017-03-22       Impact factor: 2.883

4.  Systematic in silico Evaluation of Leishmania spp. Proteomes for Drug Discovery.

Authors:  Crhisllane Rafaele Dos Santos Vasconcelos; Antonio Mauro Rezende
Journal:  Front Chem       Date:  2021-04-27       Impact factor: 5.221

5.  Novel 5-(nitrothiophene-2-yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity against promastigote stage of Leishmania major.

Authors:  Seyed Esmail Sadat-Ebrahimi; Maryam Mirmohammadi; Zahra Mojallal Tabatabaei; Marjan Azimzadeh Arani; Sogol Jafari-Ashtiani; Mahsa Hashemian; Parham Foroumadi; Azadeh Yahya-Meymandi; Setareh Moghimi; Mohammad Hassan Moshafi; Peiman Norouzi; Susan Kabudanian Ardestani; Alireza Foroumadi
Journal:  Iran J Pharm Res       Date:  2019       Impact factor: 1.696

  5 in total

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