134226-79-2Relevant academic research and scientific papers
Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12
Wiedeman, Paul E.,Fesik, Stephen W.,Petros, Andrew M.,Nettesheim, David G.,Mollison, Karl W.,Lane, Benjamin C.,Or, Yat Sun,Luly, Jay R.
, p. 4456 - 4461 (1999)
C24-Deoxyascomycin was prepared in a two-step process from ascomycin and evaluated for its immunosuppressant activity relative to ascomycin and FK506. An intermediate in the synthetic pathway, Δ23,24-dehydroascomycin, was likewise evaluated. De
ANTIFUNGAL COMPOUNDS
-
Paragraph 00109, (2015/07/23)
The technical field of the invention is in pharmaceutical compounds, combinations and methods. In an aspect, the disclosure provides macrolide compounds and combinations with a second active agent, suitable for use as antifungal therapies, as well as methods for their use and compositions containing the same. Macrolide compounds include epimers of FK506 and related analogs.
Regioselective carbon-carbon bond formation in the effector domain of ascomycin
Horvath, Amarylla,Grassberger, Maximilian A,Schulz, Gerhard,Haidl, Ewald,Sperner, Hildegard,Steck, Andrea
, p. 7469 - 7476 (2007/10/03)
Starting from 33-O-silyl-protected ascomycin or its 23,24-dehydration product, regio- and stereo-selective formal aldol reactions under carbon-carbon bond formation at C-22, C-23, or C-24 are demonstrated. Additionally, with the 22-silyl enol ether ascomycin derivative a rhodium(I)-catalysed shift of the 19,20 double bond into the 19,38 exocyclic position is observed at elevated temperature. (C) 2000 Elsevier Science Ltd.
C32-amino derivatives of the immunosuppressant ascomycin
Ok, Hyun O.,Szumiloski, John L.,Beattie, Thomas R.,Goulet, Mark T.,Staruch, Mary Jo,Dumont, Francis J.,Wyvratt, Matthew J.
, p. 2199 - 2204 (2007/10/03)
Various C32-amino derivatives were investigated as replacements for the C32-hydroxyl group of ascomycin and its C24-deoxy analog. The syntheses of these amino derivatives and their biological evaluation are reported herein.
