Utility of amino acid coupled 1,2,4-triazoles in organic synthesis: synthesis of some new antileishmainal agents

Starting from 3-amino-5-(2-hydroxyphenyl) amino acid coupled triazoles 1a-e, new 3-(2-hydroxyphenyl)-3H-imidazo[2,1-c][1,2,4]triazol-6(5/f)-one 2a,b, 3b,d, 6a and 3-N-arly(alkyl) amino acid coupled triazoles 4b,d, 7a,c,d,e have been synthesized as potential antileishmanial agents. The structures of...

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Bibliographic Details
Published in:Bulletin of the Chemical Society of Ethiopia Vol. 32; no. 3; p. 559
Main Authors: Saghier, Ahmed M.M. El, Mohamed, Mounir A.A, Abdalla, Omayma A, Kadry, Asmaa M
Format: Journal Article
Language:English
Published: Chemical Society of Ethiopia 01-01-2018
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Summary:Starting from 3-amino-5-(2-hydroxyphenyl) amino acid coupled triazoles 1a-e, new 3-(2-hydroxyphenyl)-3H-imidazo[2,1-c][1,2,4]triazol-6(5/f)-one 2a,b, 3b,d, 6a and 3-N-arly(alkyl) amino acid coupled triazoles 4b,d, 7a,c,d,e have been synthesized as potential antileishmanial agents. The structures of the newly synthesized compounds were confirmed using elemental and spectral analyses (FT-IR, [.sup.1]H-NMR, [.sup.13]C-NMR and MS). The in vitro antileishmanial potency of the synthesized compounds was evaluated compared to Amphotericin B deoxycholate and miltefosine as lead references. Compounds 2b, 7d and 7e showed perfect I[C.sub.50] values corresponding to amphotericin B and more patent than miltefosine against L. aethiopica promastigotes.KEY WORDS: Amino acids, Coupled, Imidazo-1,2,4-Triazole, Promatigote, Antileishmanial
ISSN:1011-3924
1726-801X
DOI:10.4314/bcse.v32i3.14