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Synthesis, structure, toxicological and pharmacological investigations of 4-hydroxycoumarin derivatives.

Abstract：

:Twenty 4-hydroxycoumarin derivatives were synthesized. Five of them are described for the first time. The X-ray crystal structure analysis of 3,3'-(2,3,4-trimethoxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (7) and 3,3'-(3,5-dimethoxy-4-hydroxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (9) confirmed the structure of these compounds. A comparative pharmacological study of the anticoagulant effect with respect to Warfarin showed that the synthesized compounds have different anticoagulant activities. The most prospective compound is 3,3'-(4-chlorophenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (12) with low toxicity, very good index of absorption and dose dependent anticoagulant activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Manolov I,Maichle-Moessmer C,Danchev N

doi

10.1016/j.ejmech.2006.03.007

subject

Has Abstract

pub_date

2006-07-01 00:00:00

pages

882-90

issue

7

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(06)00097-3

journal_volume

41

pub_type

杂志文章

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