Oligoamides of 2-amino-5-alkylthiazole 4-carboxylic acids: anti-trypanosomal compounds

Stuart Lang, Abedawn I Khalaf, David Breen, Judith Huggan, Carol Clements, Simon MacKay, Colin Suckling

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

A range of minor groove binders (MGBs) and the intermediates formed in their synthesis was screened against infectious agents including bacteria and parasites. Activity was found against Trypanosoma brucei. Of particular interest is a molecule which does not contain a typical basic flexible tail group found in MGBs, but instead has an unprotected carboxylic acid group at that position (compound 4), which has activity of 63 nM against T. brucei.

LanguageEnglish
Pages1170-1179
Number of pages10
JournalMedicinal Chemistry Research
Volume23
Issue number3
Early online date28 Aug 2013
DOIs
Publication statusPublished - 2014

Fingerprint

Trypanosoma brucei brucei
Carboxylic Acids
Binders
Tail
Bacteria
Parasites
Molecules

Keywords

  • DNA
  • minor groove binder
  • amide
  • thiazole
  • anti-parasitic activity

Cite this

Lang, Stuart ; Khalaf, Abedawn I ; Breen, David ; Huggan, Judith ; Clements, Carol ; MacKay, Simon ; Suckling, Colin. / Oligoamides of 2-amino-5-alkylthiazole 4-carboxylic acids : anti-trypanosomal compounds. In: Medicinal Chemistry Research. 2014 ; Vol. 23, No. 3. pp. 1170-1179.
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Oligoamides of 2-amino-5-alkylthiazole 4-carboxylic acids : anti-trypanosomal compounds. / Lang, Stuart; Khalaf, Abedawn I; Breen, David; Huggan, Judith; Clements, Carol; MacKay, Simon; Suckling, Colin.

In: Medicinal Chemistry Research, Vol. 23, No. 3, 2014, p. 1170-1179.

Research output: Contribution to journalArticle

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