Synthetic studies on leupeptins and their analogs.
نویسندگان
چکیده
Leupeptins, fermentation products of various strains of Actinomycetes^ showed strong antiplasmin activity2) and were identified as being a mixture of two major components, leupeptin Ac-LL (acetyl-L-leucyl-L-leucyl-DL-argininal, 1) and leupeptin Pr-LL (propionyl-L-leucyl-L-leucyl-DL-argininal, 2), and their analogs containing isoleucine or valine in place of one or two leucine residues of 1 or 2.3>4) Chemical synthesis of leupeptin Ac-LL and Pr-LL was carried out by the oxidation of the corresponding argininol derivatives^ to confirm the proposed structures. The analo-
منابع مشابه
Biological activities of leupeptins.
Leupeptins, leupeptin Pr and leupeptin Ac, strongly inhibit proteolysis by plasmin, trypsin and papain, but do not inhibit proteolysis by <#-chymotrypsin. The inhibition is competitive with substrates. The inhibitory effect on esterolysis by plasmin and trypsin is weaker than on proteolysis. The results with derivatives of leupeptins which contain carboxyl or alcohol instead of aldehyde and of ...
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عنوان ژورنال:
- The Journal of antibiotics
دوره 25 9 شماره
صفحات -
تاریخ انتشار 1972