Modification of the clozapine structure by parallel synthesis.
A structure-activity study based on the core structure of clozapine 1b was accomplished by utilizing high-throughput synthesis. Several focused libraries were designed and synthesized to quickly develop SAR. The results indicate that by varying different regions of clozapine, both D(1)-selective and D(2)-selective compounds can be obtained.
Su
Jing
J
Department of Chemical Research, Schering-Plough Research Institute K15 2545, Kenilworth, NJ 07033, USA. jing.su@spcorp.com
Tang
Haiqun
H
McKittrick
Brian A
BA
Burnett
Duane A
DA
Zhang
Hongtao
H
Smith-Torhan
April
A
Fawzi
Ahmad
A
Lachowicz
Jean
J
D003024:Clozapine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D015394:Molecular Structure; D017447:Receptors, Dopamine D1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D013329:Structure-Activity Relationship
D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D003024:Clozapine