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8-Aminoquinolines as anticoccidials--II

R E Armer1, J S Barlow, C J Dutton

  • 1Animal Health Discovery, Pfizer Central Research, Sandwich, Kent, U.K.

Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
PubMed
Summary
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Researchers investigated pentaquine

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Biochemistry

Background:

  • Pentaquine is an antimalarial drug.
  • Its mechanism of action in chickens is not fully understood.
  • Novel analogues with improved activity are sought.

Purpose of the Study:

  • To investigate the in vivo mechanism of action of pentaquine in chickens.
  • To identify the active metabolite of pentaquine.
  • To synthesize and evaluate novel pentaquine analogues.

Main Methods:

  • Metabolic studies of pentaquine using monoamine oxidase.
  • Synthesis of pentaquine derivatives (oxime, acetal, ketal).
  • In vitro testing of synthesized compounds for anticoccidial activity.

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Main Results:

  • Pentaquine aldehyde was proposed as the likely active metabolite.
  • The unstable pentaquine aldehyde could not be isolated.
  • Synthesized oxime and cyclic acetal/ketal derivatives exhibited in vitro anticoccidial activity.

Conclusions:

  • Pentaquine aldehyde is likely the active metabolite responsible for anticoccidial effects.
  • Novel derivatives of pentaquine show promise as anticoccidial agents.
  • Further research into these derivatives could lead to improved treatments.