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Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Apr 01; Vol. 18 (7), pp. 2272-6. Date of Electronic Publication: 2008 Mar 07. - Publication Year :
- 2008
-
Abstract
- Taking advantage of the structural features of natural products showing anti-trypanosomatid activity, we designed and synthesized a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives. The library was obtained following a parallel approach and using readily available synthons. All the derivatives showed inhibitory activity toward either Trypanosoma or Leishmania species, with 8, 10, and 16 being the most active compounds against Trypanosoma brucei rhodesiense, Leishmania donovani, and Trypanosoma cruzi cells (IC(50)=50nM, IC(50)=0.28microM, and IC(50)=1.26microM, respectively).
- Subjects :
- Animals
Anthraquinones chemical synthesis
Antiprotozoal Agents chemical synthesis
Inhibitory Concentration 50
Models, Chemical
Naphthoquinones chemical synthesis
Parasitic Sensitivity Tests
Anthraquinones pharmacology
Antiprotozoal Agents pharmacology
Drug Design
Leishmania drug effects
Naphthoquinones pharmacology
Trypanosoma drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18353643
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.03.009