Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry
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- 作者：Chris D. Edlin ; Garreth Morgans ; Susan Winks ; Sandra Duffy ; Vicky M. Avery ; Sergio Wittlin ; David Waterson ; Jeremy Burrows ; Justin Bryans
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：July 12, 2012
- 年：2012
- 卷：3
- 期：7
- 页码：570-573
- 全文大小：284K
- 年卷期：v.3,no.7(July 12, 2012)
- ISSN：1948-5875
文摘
Triage of a set of antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite Plasmodium falciparum strains identified several novel chemotypes suitable for hit-to-lead chemistry investigation. The set was further refined through investigation of their in vitro ADME properties, which identified templates with good potential to be developed further as antimalarial agents. One example was profiled in an in vivo murine Plasmodium berghei model of malaria infection.