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Aliphatic propargylamines: New antiapoptotic drugs
Author(s) -
Boulton Alan A.,
Davis Bruce A.,
Durden David A.,
Dyck Lillian E.,
Juorio Augusto V.,
Li XinMin,
Paterson I. Alick,
Yu Peter H.
Publication year - 1997
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/(sici)1098-2299(199711/12)42:3/4<150::aid-ddr6>3.0.co;2-p
Subject(s) - in vivo , bioavailability , chemistry , pharmacokinetics , pharmacology , monoamine oxidase , drug , in vitro , monoamine oxidase b , monoamine neurotransmitter , combinatorial chemistry , stereochemistry , biochemistry , medicine , biology , receptor , enzyme , microbiology and biotechnology , serotonin
Two series of drugs, the aliphatic‐N‐methyl propargylamines and the aliphatic propargylamines, have been synthesised and shown to be specific, irreversible, and potent monoamine oxidase B inhibitors and neural rescue agents. In the latter case, an absolute stereochemical requirement for the R isomer exists. Both series of compounds have been shown, in numerous in vitro and in vivo experimental paradigms, to be effective neuronal rescue agents. Candidates from both series exhibit excellent bioavailability and pharmacokinetics and offer opportunities for treating neurodegenerative disorders and stroke and cognitive decline in companion animals. Drug Dev. Res. 42:150–156, 1997. © 1997 Wiley‐Liss, Inc.