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Novel 21-aminosteroids that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma.

Abstract：

:A novel class of 21-aminosteroids has been developed. Compounds within this series are potent inhibitors of iron-dependent lipid peroxidation in rat brain homogenates with IC50's as low as 3 microM. Furthermore, selected members enhance early neurological recovery and survival in a mouse head injury model. Significant improvement in the 1 h post-head-injury neurological status (grip test score) by as much as 168.6% of the control has been observed. The most efficacious compound in this assay (30) showed an increase in the 1-week survival of 78.6% as compared to 27.3% for the vehicle-treated mice in the head-injury model. Based on its biological profile, 21-[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]-16 alpha- methylpregna-1,4,9(11)-triene-3,20-dione monomethanesulfonate (30) was selected for further evaluation and is currently entering phase I clinical trials for the treatment of head and spinal trauma.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Jacobsen EJ,McCall JM,Ayer DE,Van Doornik FJ,Palmer JR,Belonga KL,Braughler JM,Hall ED,Houser DJ,Krook MA

doi

10.1021/jm00166a010

subject

Has Abstract,Author List Incomplete

pub_date

1990-04-01 00:00:00

pages

1145-51

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

33

pub_type

杂志文章

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