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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
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
Institution:Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. frank.bennett@spcorp.com
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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