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Antileishmanial actions of tricyclic neuroleptics appear to lack structural specificity

Authors
  • Evans, A.Tudor
  • Croft, Simon L.
Type
Published Article
Journal
Biochemical Pharmacology
Publisher
Elsevier
Publication Date
Jan 01, 1994
Accepted Date
Mar 30, 1994
Volume
48
Issue
3
Pages
613–616
Identifiers
DOI: 10.1016/0006-2952(94)90293-3
Source
Elsevier
Keywords
License
Unknown

Abstract

There is continuing interest in the antimicrobial effects of tricyclic neuroleptics and antidepressants, particularly against trypanosomatid protozoa, but few studies have attempted to dissociate antiparasitic actions from effects on the central nervous system. In this report, we have measured the antileishmanial potency of a range of structural analogues in this drug group, and conclude that no one structural determinant is critical for activity. Instead, potency may be predicted from an overall determination of the lipophilic and steric components of the structure by a simple combination of two descriptive parameters, valence connectivity and an interactive term.

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