| 摘要 |
<p>Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: wherein Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, or RHN(CH2)n-; n is the integer 3 or 4; each R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or , wherein R2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, -NR4R5 wherein each of R4 and R5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or wherein R1 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is RHN(CH2)nand each R is hydrogen; with the provisos that when Z is .beta.-benzylthioethyl or S-(5'-desoxyadenosin-5'-yl)-S-methyl-thioethyl, R is hydrogen and R1 is hydroxy, when Z is .gamma.guanidinopropyl, R is hydrogen and R1 is hydroxy or a straight or branched lower alkoxy group of from 1 to 8 carbon atoms, and when Z is RHN(CH2)n- both R groups are the same; and pharmaceutically acceptable salts and individual optical isomers thereof.</p> |
