ALIPHATIC PROPARGYLAMINES - NEW ANTIAPOPTOTIC DRUGS

Two series of drugs, the aliphatic-N-methyl propargylamines and the al iphatic propargylamines, have been synthesised and shown to be specifi c, irreversible, and potent monoamine oxidase B inhibitors and neural rescue agents. In the latter case, an absolute stereochemical requirem ent for the R isomer exists. Both series of compounds have been shown, in numerous in vitro and in vivo experimental paradigms, to be effect ive neuronal rescue agents. Candidates from both series exhibit excell ent bioavailability and pharmacokinetics and offer opportunities for t reating neurodegenerative disorders and stroke and cognitive decline i n companion animals. (C) 1997 Wiley-Liss, Inc.