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

Frank Bennett,Anil K Saksena,Raymond G Lovey,Yi-Tsung Liu,Naginbhai M Patel,Patrick Pinto,Russel Pike,Edwin Jao,Viyyoor M Girijavallabhan,Ashit K Ganguly,David Loebenberg,Haiyan Wang,Anthony Cacciapuoti,Eugene Moss,Fred Menzel,Roberta S Hare,Amin Nomeir

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

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.

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关键词

Antifungal,Posaconazole

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