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Studies on an immunosuppressive macrolactam, ascomycin: synthesis of a C-33 hydroxyl derivative
M Kawai1, I W Gunawardana, K W Mollison
1Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
Ascomycin 2, a close analogue of the immunosuppressant FK506 1, was modified to incorporate a hydroxyl group at the C-33 position. This increased the aqueous solubility of ascomycin by a hundred-fold at pH 7.4 and by approximately 300-fold at pH 6.5. Ascomycin 3 also exhibited an excellent immunosuppressive activity in vitro, as tested in a human mixed lymphocyte proliferation (HuMLR) assay, and in vivo using a rat popliteal lymph node (rPLN) hyperplasia assay.