Abstract:
:1-(3'-Diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines were synthesized and evaluated for CQ-resistant reversal activity. In general the compounds of the series elicit better biological response than their phenylmethyl analogues. The most active compound 4b has been evaluated in vivo in detail, and the results are presented. The possible mode of action of the compounds of this series is by inhibition of the enzyme heme oxygenase, thereby increasing the levels of heme and hemozoin, which are lethal to the parasite.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Batra S,Srivastava P,Roy K,Pandey VC,Bhaduri APdoi
10.1021/jm000083ukeywords:
subject
Has Abstractpub_date
2000-09-07 00:00:00pages
3428-33issue
18eissn
0022-2623issn
1520-4804pii
jm000083ujournal_volume
43pub_type
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pub_type: 杂志文章
doi:10.1021/jm00159a013
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pub_type: 杂志文章
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更新日期:2013-08-08 00:00:00
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pub_type: 杂志文章
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更新日期:2004-12-16 00:00:00
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更新日期:2007-06-14 00:00:00
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pub_type: 杂志文章
doi:10.1021/jm00376a003
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abstract::During the course of our investigations in the oxazolidinone antibacterial agent area, we have identified a subclass with especially potent in vitro activity against mycobacteria. The salient structural feature of these oxazolidinone analogues, 6 (U-100480), 7 (U-101603), and 8 (U-101244), is their appended thiomorpho...
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abstract::Primaquine (I) has been extensively used in combination with other drugs in the radical cure of relapsing malaria as well as for prophylaxis or the interruption of transmission. This, coupled with the activity data reported for 4-methylprimaquine (II), has led to the synthesis of a series of 14 4-substituted analogues...
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abstract::Fyn is a member of the Src-family of nonreceptor protein-tyrosine kinases. Its abnormal activity has been shown to be related to various human cancers as well as to severe pathologies, such as Alzheimer's and Parkinson's diseases. Herein, a structure-based drug design protocol was employed aimed at identifying novel F...
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abstract::Following erythrocyte invasion, malaria parasites export a catalogue of remodeling proteins into the infected cell that enable parasite development in the human host. Export is dependent on the activity of the aspartyl protease, plasmepsin V (PMV), which cleaves proteins within the Plasmodium export element (PEXEL; Rx...
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00246a020
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