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

被引:27
作者
Bennett, F [1 ]
Saksena, AK [1 ]
Lovey, RG [1 ]
Liu, YT [1 ]
Patel, NM [1 ]
Pinto, P [1 ]
Pike, R [1 ]
Jao, E [1 ]
Girijavallabhan, VM [1 ]
Ganguly, AK [1 ]
Loebenberg, D [1 ]
Wang, HY [1 ]
Cacciapuoti, A [1 ]
Moss, E [1 ]
Menzel, F [1 ]
Hare, RS [1 ]
Nomeir, A [1 ]
机构
[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA
关键词
antifungal; posaconazole;
D O I
10.1016/j.bmcl.2005.09.031
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:186 / 190
页数:5
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