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Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Jan 01; Vol. 16 (1), pp. 186-90. Date of Electronic Publication: 2005 Nov 02. - Publication Year :
- 2006
-
Abstract
- As part of a detailed study, the syntheses, biological activities, and pharmacokinetic properties of hydroxylated analogues of the previously described broad spectrum antifungal agents, Sch 51048 (1), Sch 50001 (3), and Sch 50002 (4), are described. Based on an overall superior profile, one of the alcohols, Sch 56592 (2), was selected for clinical studies.
- Subjects :
- Alcohols
Animals
Antifungal Agents chemistry
Aspergillosis drug therapy
Candidiasis drug therapy
Dose-Response Relationship, Drug
Drug Design
Drug Evaluation, Preclinical
Haplorhini
Humans
Immunosuppressive Agents pharmacology
Mice
Models, Chemical
Time Factors
Triazoles pharmacokinetics
Antifungal Agents pharmacology
Chemistry, Pharmaceutical methods
Triazoles chemical synthesis
Triazoles chemistry
Triazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16260134
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.09.031