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Synthesis and antileishmanial activity of 6-methoxy-4-methyl-N-[6-(substituted-1-piperazinyl)hexyl]-8-quinolinamines and related compounds.

Authors
  • Johnson, J L
  • Werbel, L M
Type
Published Article
Journal
Journal of medicinal chemistry
Publication Date
Feb 01, 1983
Volume
26
Issue
2
Pages
185–194
Identifiers
PMID: 6827535
Source
Medline
License
Unknown

Abstract

The 8-quinolinamine, 4-[6-[6-methoxy-4-methyl-8-quinolinyl)amino]hexyl]-1-piperazineethanol (1b), has been shown to be highly effective against Leishmania donovani infections in hamsters. In an effort to obtain a more potent, less toxic 8-quinolinamine, a series of analogues (2) was prepared that examined particularly the structural requirements of the terminal piperazine moiety. Of the substituted piperazines and alternative heterocycles prepared, as well as those quinoline analogues with ring insertion of a methyl group in the 2-position or an aryloxy substituent in the 5-position, an increase in potency was achieved only with the 2-hydroxypropyl analogue (2f).

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