Structure-Activity Relationships of the Butyrophenones and Diphenylbutylpiperidines

摘要: Shortly after the synthesis (Charpentier, 1950) and pharmacological evaluation of chlorpromazine (Courvoisier et al., 1952), this phenothiazine derivative was recognized to be a most useful antipsychotic agent in clinic (Delay 1952). The discovery chlorpromazine, together with rediscovery action reserpine (Bein, 1953; Kline, 1954), triggered an enormous research effort many laboratories throughout world. These two structurally very different types neuroleptics served as leads for preparation subsequent investigation tremendous amount synthetic derivatives. Many them showed similar profiles, but few were superior original leads. However, it not until butyrophenones by Janssen al. (1959a) that different, although pharmacologically clinically similar, type found.