Antimalarial agents IX. 3-alkylquinolones as potential repository drugs

✍ Scribed by J. H. Burckhalter; Douglas G. Mikolasek

• Book ID: 102395324
• Publisher: John Wiley and Sons
• Year: 1967
• Tongue: English
• Weight: 388 KB
• Volume: 56
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600560218

✦ Synopsis

As a possible answer to the need for antimalarials with more prolonged activity as well as for drug resistant malaria, several compounds related structurally to endochin (11) have been synthesized. They failed to pass preliminary pharmacological requirements.

LTHOUGH the 4-aminoquinoline antimalarial

A agents, chloroquine and amodiaquine, are generally effective suppressive agents in areas of endemic malaria, they must be readministered every few weeks to maintain therapeutic effectiveness ( ). An objective of the present study is the synthesis of certain substituted quinolines which might show prolonged antimalarial activity. Should such agents be found, i t is hoped that prolonged activity might also contribute effectiveness against the recent serious threat posed by resistant falcipamm malaria (2).

Discussion

Compound I (SN-10,275) (3) once gave promise of possessing prolonged activity because 1 to 5% of the drug was still present in the plasma as long as 3 months following the last dose (4). However, photosensitivity manifest by severe itching prohibits administration to humans.