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新型[1,3]噻唑并[4,5-d]哒嗪-4(5H)-酮的合成与生物活性

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

作者信息

Demchenko Anatoly, Bobkova Ludmila, Yadlovskiy Oleh, Buchtiarova Tatiana, Demchenko Sergey

机构信息

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

出版信息

Sci Pharm. 2016 Apr-Jun;84(2):255-68. doi: 10.3797/scipharm.1505-16. Epub 2015 Aug 27.

DOI:10.3797/scipharm.1505-16
PMID:27222602
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4871179/
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 (1)H-NMR, (13)C-NMR spectroscopy, and liquid chromatography-mass spectrometry.

摘要

通过5-苯甲酰基（α-呋喃甲酰基或α-噻吩甲酰基）-2-氨基取代的噻唑-4-羧酸甲酯9a-c、13a-e与肼反应，以78-87%的产率合成了一系列新型的2-（N-吡咯烷基、N-哌啶基或N-吗啉基）-7-苯基（α-呋喃甲酰基或α-噻吩甲酰基）-[1,3]噻唑并[4,5-d]哒嗪酮10a-c、14-16a、b。已对这些新化合物的体内镇痛和抗炎活性进行了测试。所有化合物均通过（1）H-NMR、（13）C-NMR光谱和液相色谱-质谱进行了表征。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/163901a6d3e1/SciPharm-84-255-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/f1444580c29d/SciPharm-84-255-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/3c0e989b3043/SciPharm-84-255-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/19383b9079da/SciPharm-84-255-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/163901a6d3e1/SciPharm-84-255-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/f1444580c29d/SciPharm-84-255-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/3c0e989b3043/SciPharm-84-255-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/19383b9079da/SciPharm-84-255-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8b/4871179/163901a6d3e1/SciPharm-84-255-g004.jpg

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