Synthesis and Biological Activity of Silyl- and Germylsubstituted Trifluroacetylfurans

نویسندگان

  • Luba Ignatovich
  • Dzintra Zarina
  • Irina Shestakova
  • Skaidrite Germane
  • Edmunds Lukevics
چکیده

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)).

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and characterization of novel silyl derivatives of curcumin

Abstract:Turmeric is a member of the ginger family (Zingiberaceae), which is extensively used as a spice, food preservative and colouring material. Curcumin is a main bioactive natural compound derived from the rhizome of this plant. Curcumin can exist in several tautomeric forms, keto and enol. The keto form is more stable than enol form. Silyl ethers have proven to be versatile substrates for...

متن کامل

Synthesis, Characterization, and Biological Activity Studies on Fanlizhicyclopeptide A

The synthesis of a proline-rich cyclic heptapeptide, fanlizhicyclopeptide A (8), previouslyisolated from the fruits of Annona squamosa (sugar-apples), is described via coupling oftetrapeptide l-prolyl-l-tyrosyl-l-leucyl-l-proline methyl ester with tripeptide Boc-glycyl-lvalyl-l-proline followed by cyclization of the linear fragment having seven amino acid units.Structure of the synthesized cycl...

متن کامل

Synthesis, Characterization, and Biological Activity Studies on Fanlizhicyclopeptide A

The synthesis of a proline-rich cyclic heptapeptide, fanlizhicyclopeptide A (8), previouslyisolated from the fruits of Annona squamosa (sugar-apples), is described via coupling oftetrapeptide l-prolyl-l-tyrosyl-l-leucyl-l-proline methyl ester with tripeptide Boc-glycyl-lvalyl-l-proline followed by cyclization of the linear fragment having seven amino acid units.Structure of the synthesized cycl...

متن کامل

Synthesis and Biological Evaluation of Thiosemicarbazide Derivatives Endowed with High Activity toward Mycobacterium Bovis

Thiosemicarbazides are potent intermediates for the synthesis of pharmaceutical and bioactive materials and thus, they are used extensively in the field of medicinal chemistry. The imine bond (-N=CH-) in these compounds are useful in organic synthesis, in particular for the preparation of heterocycles and non-natural β-aminoacids.In this paper the synthesis of some new thiosemicarbazide derivat...

متن کامل

Synthesis and Biological Evaluation of Thiosemicarbazide Derivatives Endowed with High Activity toward Mycobacterium Bovis

Thiosemicarbazides are potent intermediates for the synthesis of pharmaceutical and bioactive materials and thus, they are used extensively in the field of medicinal chemistry. The imine bond (-N=CH-) in these compounds are useful in organic synthesis, in particular for the preparation of heterocycles and non-natural β-aminoacids.In this paper the synthesis of some new thiosemicarbazide derivat...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Metal-Based Drugs

دوره 8  شماره 

صفحات  -

تاریخ انتشار 2001