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Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.

Abstract：

:Several cyclic enaminone esters were synthesized, characterized, and evaluated for anticonvulsant and antibacterial activities using standardized tests. A series of enaminones were mainly phenyl analogs of anticonvulsant enaminones, while a second series comprised of compounds bearing the oxazolidinone pharmacophoric moiety found in the synthetic antibacterial linezolid. The enaminone ester bearing an unsubstituted anilino analog showed class 2 anticonvulsant activity. This represents a first report of an unsubstituted anilino enaminone with anticonvulsant activity. The enaminone esters gave interesting UV data, and four analogs displayed potent anticonvulsant activities, while another four compounds showed moderate anticonvulsant activities. Surprisingly, none of the enaminone esters had any significant antibacterial activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Edafiogho IO,Phillips OA,Udo EE,Samuel S,Rethish B

doi

10.1016/j.ejmech.2008.07.005

subject

Has Abstract

pub_date

2009-03-01 00:00:00

pages

967-75

issue

3

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(08)00333-4

journal_volume

44

pub_type

杂志文章

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