title: Antifungal rapamycin analogues with reduced immunosuppressive activity.
abstract: Several 1,2,3,4-tetrahydro- and 7-N-hydroxycarbamate derivatives of the natural product rapamycin were prepared and assayed for their immunosuppressive and antifungal profiles. Substitutions at the 7-position indicate the possibility of a differentiated immunosuppressive to antifungal profile, whereas 40-position variants of the tetrahydro-analogues did not show similar differentiated activity.
authors.affiliation: Infectious and Immunological Diseases Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA.
authors.forename: D A
authors.initials: DA
authors.lastname: Dickman
authors.forename: H
authors.initials: H
authors.lastname: Ding
authors.forename: Q
authors.initials: Q
authors.lastname: Li
authors.forename: A M
authors.initials: AM
authors.lastname: Nilius
authors.forename: D J
authors.initials: DJ
authors.lastname: Balli
authors.forename: S J
authors.initials: SJ
authors.lastname: Ballaron
authors.forename: J M
authors.initials: JM
authors.lastname: Trevillyan
authors.forename: M L
authors.initials: ML
authors.lastname: Smith
authors.forename: L S
authors.initials: LS
authors.lastname: Seif
authors.forename: K
authors.initials: K
authors.lastname: Kim
authors.forename: A
authors.initials: A
authors.lastname: Sarthy
authors.forename: R C
authors.initials: RC
authors.lastname: Goldman
authors.forename: J J
authors.initials: JJ
authors.lastname: Plattner
authors.forename: Y L
authors.initials: YL
authors.lastname: Bennani
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D001702:Biopharmaceutics; D002175:Candida / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D015398:Signal Transduction; D020123:Sirolimus / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D007166:Immunosuppressive Agents; D020123:Sirolimus