Potential radioprotective agents--V. Melatonin analogs. Oral activity of p-aminopropiophenone and its ethylene ketal.
Seven new amides of 5-methoxytryptamine were synthesized and tested for radioprotective activity in mice. One of them, the heptafluorobutyramide 4, is moderately active (57% survivors), the rest demonstrate little or no activity. Of twelve compounds that had been found to exhibit high radioprotective activity by ip injection, only two [p-aminopropiophenone (9) and its ethylene ketal 8] retain that high activity (92-95% survivors) when administered orally. Three are moderately active: p-aminobenzonitrile (10, 55%), 5-methoxytryptamine octanoic amide (11, 50%), and p-aminobenzophenone (12, 48%).
Blickenstaff
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Richard L. Roudebush VA Medical Center, Indianapolis, IN, USA.
Reddy
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Witt
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D008735:5-Methoxytryptamine / Q000737:chemistry; D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D009682:Magnetic Resonance Spectroscopy; D008550:Melatonin / Q000031:analogs & derivatives*; D051379:Mice; D008815:Mice, Inbred Strains; D011427:Propiophenones / Q000737:chemistry / Q000494:pharmacology*; D011837:Radiation-Protective Agents / Q000378:metabolism / Q000494:pharmacology*
D000577:Amides; D011427:Propiophenones; D011837:Radiation-Protective Agents; D008735:5-Methoxytryptamine; C029564:4-aminopropiophenone; D008550:Melatonin