Synthesis of Dibenzofuranone-Oxime Derivatives with Anticonvulsant, Antihypoxic, and Anti-Ischemic Activity

Autor:	T. A. Voronina, G. V. Mokrov, T. A. Gudasheva, I. S. Kutepova, L. A. Zhmurenko, L. N. Nerobkova, A. G. Rebeko, S. A. Litvinova
Rok vydání:	2020
Předmět:	Pharmacology Aromatic acid 010405 organic chemistry medicine.medical_treatment Pharmacology toxicology Oxime 01 natural sciences Medicinal chemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry Maximal electroshock chemistry.chemical_compound Anticonvulsant chemistry Active compound Drug Discovery Ischemic stroke medicine
Zdroj:	Pharmaceutical Chemistry Journal. 53:997-1004
ISSN:	1573-9031 0091-150X
DOI:	10.1007/s11094-020-02112-2
Popis:	New dibenzofuranone-oxime derivatives were designed based on active structures of oxime esters. Compounds of the proposed group were synthesized using 3,4,6,7,8,9-hexahydrodibenzo[b,d]furan-1(2H)-one oxime and aromatic acid chlorides. The anticonvulsant activity of the new compounds was studied. The structure— activity relationship was analyzed. Compound 1a [3,4,6,7,8,9-hexahydrodibenzo[b,d]furan-1(2H)-one O-(3,4-dichlorobenzoyl)oxime] was the most active compound after i.p. injection to mice in the maximal electroshock test over a wide dose range of 20 – 100 mg/kg. Compound 1a at doses of 10 and 30 mg/kg exhibited antihypoxic activity in a hypoxia test with hypercapnia in a hermetic chamber and anti-ischemic activity at a dose of 10 mg/kg in a rat ischemic stroke model.
Databáze:	OpenAIRE
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