Synthesis and Biological Activity of New [1,3]Thiazolo[4,5-d]pyridazin-4(5H)-ones

Anatoly DEMCHENKO; Ludmila BOBKOVA; Oleh YADLOVSKIY; Tatiana BUCHTIAROVA; Sergey DEMCHENKO

doi:10.3797/scipharm.1505-16

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Article

27 August 2015

Synthesis and Biological Activity of New [1,3]Thiazolo[4,5-d]pyridazin-4(5H)-ones

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Institute of Pharmacology and Toxicology, Eugene Pottier 14, 03057 Kiev, Ukraine

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Sci. Pharm.2016, 84(2), 255-268;https://doi.org/10.3797/scipharm.1505-16

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Abstract

A series of novel 2-(N-pyrrolidino, N-piperidino or N-morpholino)-7-phenyl(α-furoyl or α-thienyl)-[1,3]thiazolo[4,5-d]pyridazinones 10a-c, 14-16a,b was synthesized in 78-87% yields via the reaction of methyl 5-benzoyl(α-furoyl or α-thienyl)-2-aminosubstituted-thiazol-4-carboxylates 9a-c, 13a-e with hydrazine. These new compounds have been tested for their in vivo analgesic and anti-inflammatory activities. All compounds have been characterized by ¹H-NMR, ¹³C-NMR spectroscopy, and liquid chromatography-mass spectrometry.

Keywords:

[1,3]Thiazolo[4,5-d]pyridazinones; Anti-inflammatory activity; Anаlgеsic activity; In vivo tests;«Hot plate» model; «Acetic acid cramps» model

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