Synthesis and Biological Activity of Silyl‐ and GermylsubstitutedTrifluroacetylfurans
Author(s) -
Л. Игнатович,
Dzintra Zarina,
Irīna Shestakova,
S. K. Germane,
E. Lukevics
Publication year - 2001
Publication title -
metal-based drugs
Language(s) - English
Resource type - Journals
ISSN - 0793-0291
DOI - 10.1155/mbd.2001.211
Subject(s) - silylation , computational biology , chemistry , biology , biochemistry , catalysis
A series of silyl, germyl and alkyl substituted trifluoroacetylfurans has been synthesized under Friedel-Crafts electrophilic acylation conditions. Biological investigations have demonstrated that germyl derivatives of trifluoroacetylfuran are more toxic than the silicon analogues. 5-Triethylgermyl-2- trifluoroacetylfuran was the most toxic compound (CD(nabla), 11.2 mg kg(-1), i.p. for white mice), 200 times more toxic than the silicon analogue. 5-t-Butyl- and 5-trimethylsilyl-2-trifluroacetylfuran prolong the duration of ethanol anaesthesia by 220 and 140%. 5-Triethylgermyl-2-trifluroacetylfuran exibited high anesthetic activity in hexobarbital test (prolonged the duration by 137%). Some of compounds influenced muscle tone and locomotor coordination parameters. 5-Triethylgermyl-2-trifluomacetylfuran exibited analgesic activity (D(nabla), 0.9 mg k}(-infinity)).
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