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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 01期

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.

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页码：186 / 190

页数：5

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