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Related Experiment Video

Updated: Jul 19, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives

Facile Preparation of 4-Substituted Quinazoline Derivatives

Published on: February 15, 2016

8-aminoquinolines as anticoccidials - Part III.

R E Armer¹, J S Barlow, N Chopra

¹Animal Health Discovery, Pfizer Central Research, Kent.

Bioorganic & Medicinal Chemistry Letters

|September 7, 1999

Summary

Researchers developed new pentaquine analogues with varied side-chains to combat coccidiosis. Some novel compounds showed improved anticoccidial efficacy in vitro and in vivo compared to the original drug.

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Area of Science:

Medicinal Chemistry
Parasitology
Veterinary Medicine

Background:

Coccidiosis is a significant parasitic disease affecting livestock and poultry.
Pentaquine (1) is an established antimalarial drug with potential anticoccidial properties.
Optimizing pentaquine analogues could lead to more effective coccidiosis treatments.

Purpose of the Study:

To synthesize and evaluate novel analogues of pentaquine.
To investigate the impact of side-chain modifications at the 8-amino position on anticoccidial activity.
To identify analogues with superior efficacy compared to pentaquine.

Main Methods:

Synthesis of pentaquine analogues with varied inter-nitrogen distances and terminal amino groups.
In vitro evaluation of anticoccidial activity.
In vivo testing of anticoccidial efficacy in relevant animal models.

Main Results:

Several novel pentaquine analogues were successfully synthesized.
New analogues demonstrated anticoccidial activity in vitro.
Selected analogues exhibited in vivo anticoccidial efficacy comparable or superior to pentaquine.

Conclusions:

Modification of the 8-amino side-chain of pentaquine can yield potent anticoccidial agents.
Novel analogues show promise for the treatment and prevention of coccidiosis.
Further research into these analogues could lead to new veterinary therapeutics.