Potential radioprotective agents. 2. Substituted anilines.
A series of substituted anilines was examined for radioprotective activity by injecting them ip into mice subjected to a near-lethal dose of 6 mV photons. Electronegative groups such as Br, NO2, CN, and acyl in the meta or para position gave rise to highly active compounds (80-100% protection), while p-amino, methyl, amide, hydroxy, and fluoro groups decrease activity. No general correlations could be developed, however, between biological activity and a wide variety of calculated molecular parameters. The highest activity was found with p-aminobenzophenone (1), p-aminopropiophenone (2), its ethylene ketal (3), 2-amino-5-chloropyridine (35), and 5-amino-2-chloropyridine (36).
Blickenstaff
R T
RT
Richard L. Roudebush VA Medical Center, Indianapolis, IN.
Brandstadter
S M
SM
Reddy
S
S
Witt
R
R
Lipkowitz
K B
KB
D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004583:Electrons; D016166:Free Radical Scavengers; D017665:Hydroxyl Radical; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D017785:Photons; D011837:Radiation-Protective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000814:Aniline Compounds; D016166:Free Radical Scavengers; D011837:Radiation-Protective Agents; D017665:Hydroxyl Radical