Journal of
Microbiology and Antimicrobials

  • Abbreviation: J. Microbiol. Antimicrob.
  • Language: English
  • ISSN: 2141-2308
  • DOI: 10.5897/JMA
  • Start Year: 2009
  • Published Articles: 160

Full Length Research Paper

Synthesis of simple molecules prepared as arginase inhibitors and evaluated against Leishmania amazonensis

Núbia Boechat1*, Adriana S. Lages1, Osvaldo A. Santos-Filho1, Marcelo Genestra†2, Mônica M. Bastos1 and Warner B. Kover3
  1Departamento de Pesquisa e Desenvolvimento de Fármacos, Instituto de Tecnologia em Fármacos (Farmanguinhos), FIOCRUZ, Rua Sizenando Nabuco, 100, Manguinhos,Rio de Janeiro - RJ, 21041-250, Brazil. 2Departamento de Imunologia, Instituto Oswaldo Cruz (IOC), Laboratório de Bioquímica de Tripanosomatídeos, FIOCRUZ, Av. Brasil, 4365, Manguinhos, Pavilhão Leônidas Deane, 4º andar, Rio de Janeiro - RJ, 21045-900, Brazil. 3Instituto de Química, Centro de Tecnologia, Universidade Federal do Rio de Janeiro, Bloco A, Lab A-613, Cidade Universitária, Rio de Janeiro - RJ, 21949-900, Brazil. †in memory
Email: [email protected]

  •  Accepted: 11 June 2013
  •  Published: 31 July 2013

Abstract

 

In this work, we synthesized substances and evaluated the potential leishmanicidal activity. Thirty-four (34) compounds from different chemical classes were selected for a simple synthesis in overall good yields, eight of which are not described in the literature. From the 34 compounds evaluated for preliminary leishmanicidal activity, three can be considered as prototypes for the development of leishmanicidal agents. Computational chemistry calculations, including comparative modeling of the enzyme arginase from Leishmania amazonensis and a molecular docking simulation of the synthesized molecules into the active site of the model were carried out.

 

Key words: Leishmaniasis, arginase, molecular docking, thiourea, bisguanidine, amidine, biological evaluation, comparative modeling