Structure-activity relations in an imidazoline series prepared for their analgesic properties

✍ Scribed by W. Brock Neely; H. C. White; A. Rudzik

• Publisher: John Wiley and Sons
• Year: 1968
• Tongue: English
• Weight: 353 KB
• Volume: 57
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600570718

✦ Synopsis

dergo side-chain oxidations. Oxidation occurs through the stages of benzyl methyl ketone and 1-phenyl-propane-2-01 to the acid. A corresponding mechanism would be expected to occur with fenfluramine. The amphetamines also undergo ring oxidation to give the phenol. The presence of the trifluorornethyl group on the benzene ring of fenfluramine appears to prevent such oxidation. The phenolic derivative of fenfluramine was not available t o determine whether the reaction given by Axelrod would take place, but the recovery of 77 to 100% of the administered drug as fenfluramine and its two metabolites suggests that if such oxidation does occur, it can be only to a very small extent.

Previous observations (.7, 5) have indicated that fenfluramine is rapidly absorbed into the tissues and is then slowly released into the extracellular fluid. This is also indicated by the present studies. The two amines continue to be excreted over at least a 72-hr. period and during the first 48 hr. m-trifluro-Journal of Pharmaceutical Schces methylhippuric acid is excreted at an almost continuous rate.

REFERENCES

(1) Franko.