Volume 92, Issue 2
RESEARCH LETTER
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Dual‐protected amino acid derivatives as new antitubercular agents

Pedro P. de Castro

Department of Chemistry, Federal University of Juiz de Fora, Minas Gerais, Brazil

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Débora L. Campos

Department of Biological Sciences, School of Pharmaceutical Science, São Paulo State University, Araraquara, São Paulo, Brazil

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Fernando R. Pavan

Department of Biological Sciences, School of Pharmaceutical Science, São Paulo State University, Araraquara, São Paulo, Brazil

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Giovanni W. Amarante

Corresponding Author

E-mail address: giovanni.amarante@ufjf.edu.br

Department of Chemistry, Federal University of Juiz de Fora, Minas Gerais, Brazil

Correspondence

Giovanni W. Amarante, Department of Chemistry, Federal University of Juiz de Fora, Minas Gerais, Brazil.

Email: giovanni.amarante@ufjf.edu.br

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First published: 20 April 2018
Citations: 4

Abstract

Tuberculosis is an infectious disease with high incidence and growing drug‐resistant rates. In an attempt to develop new antitubercular agents, 35 compounds were synthesized, most of them bearing a carbamate and enantiopure amino acid moiety. These compounds had their activity evaluated toward a Mycobacterium tuberculosis strain (ATCC 27294) and cytotoxicity against fibroblast MRC‐5 cells (ATCC CCL‐171). Three of the prepared derivatives presented a good antimicrobial inhibition and two of them a moderate cytotoxicity. The lipophilicity seems to play a vital role in the cell growth activity, with best results for the derivatives with a higher logP.

Number of times cited according to CrossRef: 4

  • Recent Contributions of Nuclear Magnetic Resonance in Organocatalysis Mechanism Elucidation, Current Organocatalysis, 10.2174/2213337206666190328210907, 7, 1, (7-22), (2019).
  • Design and preparation of a novel prolinamide-based organocatalyst for the solvent-free asymmetric aldol reaction, Tetrahedron, 10.1016/j.tet.2019.130855, (130855), (2019).
  • Phenolic N-Monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds, European Journal of Medicinal Chemistry, 10.1016/j.ejmech.2019.111578, (111578), (2019).
  • Biologically active metabolite(s) from haemolymph of red-headed centipede Scolopendra subspinipes possess broad spectrum antibacterial activity, AMB Express, 10.1186/s13568-019-0816-3, 9, 1, (2019).

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