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5-取代-1,2,4-三唑并[4,3-a]喹唑啉衍生物的合成及抗惊厥活性 被引量:8
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作者 邓先清 肖春瑞 +1 位作者 魏成喜 全哲山 《有机化学》 SCIE CAS CSCD 北大核心 2011年第12期2082-2087,共6页
合成了5-取代-1,2,4-三唑并[4,3-a]喹唑啉衍生物2a~2q.利用最大电惊厥法(MES)和旋转棒法(Rotarod Test),以小鼠腹腔给药,分别测定了其抗惊厥活性和神经毒性.药理实验结果表明,化合物5-正庚氧基-1,2,4-三唑并[4,3-a]喹唑啉(2d)的抗惊厥... 合成了5-取代-1,2,4-三唑并[4,3-a]喹唑啉衍生物2a~2q.利用最大电惊厥法(MES)和旋转棒法(Rotarod Test),以小鼠腹腔给药,分别测定了其抗惊厥活性和神经毒性.药理实验结果表明,化合物5-正庚氧基-1,2,4-三唑并[4,3-a]喹唑啉(2d)的抗惊厥活性最强,其半数有效量ED_(50)为19.7 mg/kg,保护指数PI为6.2.由化学物质诱发的抗惊厥实验结果表明,化合物2d能对抗由戊四唑、异烟肼、硫代氨基脲和3-巯基丙酸诱发的惊厥作用,推测其抗惊厥作用是通过增强γ-aminobutyric acid(GABA)神经能系统和活化谷氨酸脱羧酶或抑制GABA转氨酶而起抗惊厥作用. 展开更多
关键词 三唑并喹唑啉 合成 抗惊厥 戊四唑 旋转棒法
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Synthesis and antimicrobial activity of 2-(3', 5'-disubstituted-indoly-2'-yl)-4H-3, 1-benzoxazin-4-ones and their derivatives
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作者 Saundane A. R. Yarlakatti Manjunatha 《Journal of Chemistry and Chemical Engineering》 2009年第12期54-59,共6页
As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-(2', 5'-disubstituted-indol-2'-yl... As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-(2', 5'-disubstituted-indol-2'-yl)-4H-3, 1-benzoxazin-4-ones (3) were synthesized from cyclocondensation of indole-2-carbonyl chlorides (2) and anthranilic acid. Compound (3) on reaction with thiosemicarbazide and o-phenylene diamine afforded the compound (4) and (6) respectively. Compound (4) subjected to intramolecular cyclization under thermal conditions above its melting point afforded the compound (5). Similarly compound (3) on fusion with o- phenylene diamine gave compound (7). Structures of these compounds were confirmed by their spectral studies. The compounds were screened for their antimicrobial activity and the results were reported. 展开更多
关键词 indole analogues henzoxazin-4-ones triazoloquinazoline benzimidazoloquinazoline antimicrobial activity
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