86963-63-5Relevant academic research and scientific papers
Pharmaceutical amides, and preparation, formulations and use of thereof
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, (2008/06/13)
Compounds of the general formula STR1 wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C1-4 alkyl, amino, C1-4 alkylamino, di-C1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C1-4 alkoxycarbonyl, amido, C1-4 alkylamido C1-4 alkoxy, C2-4 alkenyl, cyano, aminomethyl or methylsulphonyl; Ra and Rb, which may be the same or different, each represents a hydrogen or alkali metal (e.g. sodium or lithium) atom or a C1-4 (e.g. ethyl) group; m is 0 or 1; Y is a group of formula: or a group of formula: STR2 where R1 is hydrogen or methyl; R2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR3 or --NR4 R5 where R3, R4 and R5 are each hydrogen or alkyl of 1 to 4 carbon atoms (i.e. methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or t-butyl) and R3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkepalin analogues.
