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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]

2005; Elsevier BV; Volume: 16; Issue: 1 Linguagem: Inglês

10.1016/j.bmcl.2005.09.031

1464-3405

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

Microbial Natural Products and Biosynthesis

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.