| 摘要 |
<p>Substd. dipeptides of formula (I) and their salts are new. R1R2CH-NR3-X-CONH-CHR5-(CH2)y-COR6 (I) (R1 is e.g. H, alkyl, 1-8C haloalkyl, 1-8C hydroxyalkyl, 1-8C aminoalkyl, (1-8C) alkylamino-(1-8C)alkyl, di-(1-8C)alkylamino-( 1-8C)alkyl, acylamino-(1-8C)alkyl, guanidino-(1-8C)alkyl, heteroaryl, aryl, aralkyl, 1-8C mercaptoalkyl, arylthio-1-8C) alkyl, (1-8C)alkylaralkyl, alkylthio-(1-8C)alkyl, etc. or alkenyl or substd. alkyl. R2 is COOH, (1-8C)alkoxycarbonyl, aryl-(1-8C)alkoxycarbonyl, aryloxycarbonyl or P(O)(OR10)R11; R10 is H, 1-8C alkyl or benzyl; R11 is OH, alkoxy, benzyloxy, 1-8C alkyl, aryl or benzyl; R3 is H or 1-8C alkyl; X is CHR4 or N(CH2)qR4; q is 0 or 1; R4 and R5 are R1 gps., 3-9C cycloalkyl, (3-9C)cycloalkyl-(1-8C)alkyl, indolyl, indolylalkyl, adamantyl, adamantylmethyl or aminomethylphenyl-(1-8C)alkyl; y is 0-3; R6 is OH, 1-8C alkoxy or NR8R9; R8 and R9 is H, aralkyl or 1-8C alkyl; or NR8R9 is a 4- to 6-membered heterocyclic gp. opt. contg. a O or S atom, with specified provisos. (I) inhibit enkephalinases, which are known to inactivate the natural opiate receptor agonist enkephalin; on parenteral admin. to mice they potentiated the analgesic effects of intracerebrally administered D-Ala-Met-enkephalinamide. Dose is 5-100 mg/kg given every 3-8 hrs..</p> |
