9-Anilinoacridines as potential antileishmanial agents.
- Mauël J Institute of Biochemistry, University of Lausanne, Epalinges, Switzerland.
- Denny W
- Gamage S
- Ransijn A
- Wojcik S
- Figgitt D
- Ralph R
- 1993-05-01
Published in:
- Antimicrobial agents and chemotherapy. - 1993
Amsacrine
Animals
Antiprotozoal Agents
Cell Line
Humans
Leishmania tropica
Leishmaniasis, Cutaneous
Macrophages
Mice
Mice, Inbred DBA
Tumor Cells, Cultured
English
A number of 1'-substituted 9-anilinoacridines were evaluated for their activities against promastigote and amastigote forms of Leishmania major and for their toxicities to human Jurkat leukemia cells. Several compounds possessing 1'-NH-alkyl substituents produced more than 80% growth inhibition of macrophage-infected L. major amastigotes at or below a concentration of 1 microM. 1'-Hexylamino-9-anilinoacridine (compound 14) was the least toxic compound to human Jurkat cells, while it retained strong antileishmanial activity. There was a general trend for the more lipophilic compounds to show the greatest antileishmanial activity, whereas 3,6-di-NH2 substitution of the acridine nucleus reduced or eliminated activity. Some structure-activity relationships of the various compounds are discussed.
- Language
-
- English
- Open access status
- hybrid
- Identifiers
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- DOI 10.1128/aac.37.5.991
- PMID 8517726
- Persistent URL
- https://sonar.ch/global/documents/290343
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