Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].
Author:
Bennett F, Saksena AK, Lovey RG, Liu YT, Patel NM, Pinto P, Pike R, Jao E, Girijavallabhan VM, Ganguly AK, Loebenberg D, Wang H, Cacciapuoti A, Moss E, Menzel F, Hare RS, Nomeir A.
Date: 18 April 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.
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