Literature DB >> 25092697

The new pyrazolyltetrazole derivative MSN20 is effective via oral delivery against cutaneous leishmaniasis.

Viviane Dos Santos Faiões1, Maurício Silva Dos Santos2, Alice Maria Rolim Bernardino3, Edézio Ferreira Cunha-Júnior1, Marilene Marcuzzo do Canto Cavalheiro1, Eduardo Caio Torres-Santos4.   

Abstract

An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. Azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. Here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-(4'-methoxyphenyl)1H-pyrazole-4-yl]1H-tetrazole (MSN20). MSN20 showed a 50% inhibitory concentration (IC50) of 22.3 μM against amastigotes of Leishmania amazonensis and reduced significantly the parasite load in infected mice, suggesting its utility as a lead compound for the development of an oral treatment for leishmaniasis.
Copyright © 2014, American Society for Microbiology. All Rights Reserved.

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Year:  2014        PMID: 25092697      PMCID: PMC4187983          DOI: 10.1128/AAC.02874-14

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  14 in total

1.  Drug resistance in Indian visceral leishmaniasis.

Authors:  S Sundar
Journal:  Trop Med Int Health       Date:  2001-11       Impact factor: 2.622

Review 2.  Leishmaniasis--current chemotherapy and recent advances in the search for novel drugs.

Authors:  Simon L Croft; Graham H Coombs
Journal:  Trends Parasitol       Date:  2003-11

Review 3.  Development of miltefosine as an oral treatment for leishmaniasis.

Authors:  H Sindermann; J Engel
Journal:  Trans R Soc Trop Med Hyg       Date:  2006-05-26       Impact factor: 2.184

4.  Effectiveness of novel 5-(5-amino-1-aryl-1H-pyrazol-4-yl)-1H-tetrazole derivatives against promastigotes and amastigotes of Leishmania amazonensis.

Authors:  Viviane dos Santos Faiões; Leonor L Leon; Marilene M Canto-Cavalheiro; Eduardo C Torres-Santos; Alice M R Bernardino; Percilene F Vegi; Maurício S dos Santos
Journal:  Chem Biol Drug Des       Date:  2013-10-30       Impact factor: 2.817

Review 5.  Sterol 14alpha-demethylase (CYP51) as a therapeutic target for human trypanosomiasis and leishmaniasis.

Authors:  Galina I Lepesheva; Michael R Waterman
Journal:  Curr Top Med Chem       Date:  2011       Impact factor: 3.295

6.  Evidence that the high incidence of treatment failures in Indian kala-azar is due to the emergence of antimony-resistant strains of Leishmania donovani.

Authors:  R Lira; S Sundar; A Makharia; R Kenney; A Gam; E Saraiva; D Sacks
Journal:  J Infect Dis       Date:  1999-08       Impact factor: 5.226

7.  Miltefosine, an oral agent, for the treatment of Indian visceral leishmaniasis.

Authors:  T K Jha; S Sundar; C P Thakur; P Bachmann; J Karbwang; C Fischer; A Voss; J Berman
Journal:  N Engl J Med       Date:  1999-12-09       Impact factor: 91.245

Review 8.  Chemotherapy of leishmaniasis.

Authors:  Simon L Croft; Vanessa Yardley
Journal:  Curr Pharm Des       Date:  2002       Impact factor: 3.116

9.  Pentostam (sodium stibogluconate); a 50-year personal reminiscence.

Authors:  L G Goodwin
Journal:  Trans R Soc Trop Med Hyg       Date:  1995 May-Jun       Impact factor: 2.184

10.  Leishmaniasis worldwide and global estimates of its incidence.

Authors:  Jorge Alvar; Iván D Vélez; Caryn Bern; Mercé Herrero; Philippe Desjeux; Jorge Cano; Jean Jannin; Margriet den Boer
Journal:  PLoS One       Date:  2012-05-31       Impact factor: 3.240

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  1 in total

1.  Synthesis, single crystal analysis, biological and docking evaluation of tetrazole derivatives.

Authors:  Hamid Aziz; Aamer Saeed; Farukh Jabeen; Noor Ud Din; Ulrich Flörke
Journal:  Heliyon       Date:  2018-09-17
  1 in total

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