1921
Volume 4, Issue 2
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645
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Abstract

Summary

In a search for more effective amebicides, 98 substituted 8-quinolinols were tested against ; all were examined , 63 against intestinal amebiasis in rats, 14 against intestinal amebiasis in dogs, and 4 against hepatic amebiasis in hamsters.

Many of the compounds were effective and against intestinal infections, but none of those tested against hepatic infections was encouragingly effective in nontoxic doses. Consideration of the manifest structure-activity relationships showed that activity was associated with a wide variety of substituents, particularly in the 5-, 6- or 7-position of the 8-quinolinol nucleus. Many of the active compounds did not contain iodine, thus casting doubt on the existing theory that iodine is responsible for the activity of the various iodinated-8-quinolinols in clinical use as amebicides.

Although most of the compounds were less active in the presence of gastric mucin than in its absence, many of them still were active . Therefore, susceptibility to mucin binding alone does not appear to be an adequate basis for rejecting compounds at the level. Good correlation was observed between high activity and therapeutic effect .

5-Chloro-7-diethylaminomethyl-8-quinolinol proved to be one of the most promising compounds. Its chemotherapeutic effects and toxicity in several species of animals are described, and a few observations are presented on its physiological disposition in animals.

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/content/journals/10.4269/ajtmh.1955.4.224
1955-03-01
2017-11-19
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