Preparation of 4-halo-3-hydroxyanthranilates and demonstration of their inhibition of 3-hydroxyanthranilate oxygenase activity in rat and human brain tissue.
The chemical syntheses of 4-fluoro-, 4-chloro-, and 4-bromo-3-hydroxyanthranilic acids are described. Their actions as inhibitors of 3-hydroxyanthranilate oxygenase in cell-free homogenates from rat and human brain and in rat brain slices are presented.
Todd
W P
WP
Department of Chemistry, Cornell University, Ithaca, NY 14853-1301.
Carpenter
B K
BK
Schwarcz
R
R
D015095:3-Hydroxyanthranilic Acid / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000201:enzymology*; D055598:Chemical Phenomena; D002621:Chemistry; D006219:Halogens / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D008297:Male; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D051381:Rats; D011919:Rats, Inbred Strains; D013997:Time Factors; D062367:ortho-Aminobenzoates / Q000494:pharmacology*
D006219:Halogens; D062367:ortho-Aminobenzoates; D015095:3-Hydroxyanthranilic Acid; D010088:Oxidoreductases; C026382:3-hydroxyanthranilic acid oxidase