Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 ( 1), and the discovery of posaconazole [Sch 56592; 2 or ( S, S)- 5]

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 th...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006, Vol.16 (1), p.186-190
Main Authors: Bennett, Frank, Saksena, Anil K., Lovey, Raymond G., Liu, Yi-Tsung, Patel, Naginbhai M., Pinto, Patrick, Pike, Russel, Jao, Edwin, Girijavallabhan, Viyyoor M., Ganguly, Ashit K., Loebenberg, David, Wang, Haiyan, Cacciapuoti, Anthony, Moss, Eugene, Menzel, Fred, Hare, Roberta S., Nomeir, Amin
Format: Article
Language:English
Subjects:
Alcohols
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal
Antifungal agents
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Aspergillosis - drug therapy
Biological and medical sciences
Candidiasis - drug therapy
Chemistry, Pharmaceutical - methods
Dose-Response Relationship, Drug
Drug Design
Drug Evaluation, Preclinical
Haplorhini
Humans
Immunosuppressive Agents - pharmacology
Medical sciences
Mice
Models, Chemical
Pharmacology. Drug treatments
Posaconazole
Time Factors
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacokinetics
Triazoles - pharmacology
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.09.031