Water-soluble prodrugs of cyclosporine A with tailored conversion rates
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The activity of penicillin acylase has been studied in aq. and org. solvents, as free enzyme as well as immobilized within the membrane of liq.-core capsules. The activity of the enzyme is inhibited by the accumulation of the products of the hydrolysis rea ...
Cyclosporins are a family of hydrophobic cyclic undecapeptides produced by the fungus Tolypocladium niveum. The main metabolite cyclosporin A (CsA, see Scheme, R = R' = H) is the first line drug currently used to prevent rejection of organ transplants. Its ...
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Some nonenzymic epoxide-initiated polyolefin cyclisations are reported. The presented molecules are partially constrained analogues of (3S)-oxidosqualene, the natural substrate to many important cyclase enzymes. These model compounds feature a preformed C- ...
A new route for the preparation of four new indolizidines, (1R,2S,6S,7S,8aS)- and (1R,2S,6R,7R,8aS)-1,2,6,7-tetrahydroxyindolizidine (30 and 32) and (1S,2R,7S,8S,8a-R)- and (1S,2R,7R,8R,8a-R)1,2,7,8-tetrahydroxyindolizidine (44 and 46), is reported. The sy ...
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