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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
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
Summary
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.
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.
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