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抗胆碱药——9-羟基-噻吨-9-羧酸氨基烃酯类化合物的合成
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作者 吴培金 冉允章 +1 位作者 文广伶 张其楷 《军事医学》 CAS CSCD 北大核心 1989年第4期284-290,共7页
本文报道了9-羟基-噻吨-9-羧酸氨基烃酯类化合物的合成.主要中间体9-羟基-噻吨-9-羧酸系分别采用文献方法合成,还设计由噻吨酮与金属钠和CO_2一步反应而得.在所合成9个氨基烃酯类化合物中,经初步药理实验表明,多数化合物均有不同程度的... 本文报道了9-羟基-噻吨-9-羧酸氨基烃酯类化合物的合成.主要中间体9-羟基-噻吨-9-羧酸系分别采用文献方法合成,还设计由噻吨酮与金属钠和CO_2一步反应而得.在所合成9个氨基烃酯类化合物中,经初步药理实验表明,多数化合物均有不同程度的抗胆碱作用.其中化合物Ⅵ-1的抗槟榔碱震颤作用与阿托品相当,但抗流涎作用和扩瞳作用比阿托品弱. 展开更多
关键词 9-羟基-噻吨-9-羧酸 9-羟基-噻吨-9-羧酸氨基烃酯 抗胆碱化合物
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二苯并[b,e]氧(硫)杂■羟基羧酸酯类抗胆碱能化合物的构象分析 被引量:1
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作者 高守海 恽榴红 《军事医学科学院院刊》 CSCD 北大核心 1996年第2期85-87,共3页
用系统构象搜索方法计算得到了6,11二氢二苯并[b,e]氧(硫)杂11羟基11羧酸酯类抗胆碱能化合物在不同构型时的低能构象。通过对这些构象能的分析、比较,从中确定出每种化合物能量最低的优势构象,并发现在含有哌啶醇的... 用系统构象搜索方法计算得到了6,11二氢二苯并[b,e]氧(硫)杂11羟基11羧酸酯类抗胆碱能化合物在不同构型时的低能构象。通过对这些构象能的分析、比较,从中确定出每种化合物能量最低的优势构象,并发现在含有哌啶醇的羧酸酯中,酯键处于直立键时的构象能要低于处于平伏键时的构象能。 展开更多
关键词 胆碱化合物 羟基羧酸酯类 构象分析
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有机药物化学中不对称合成手性产率及其随温度变化规律的研究 被引量:1
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作者 胡文祥 崔淑华 +1 位作者 袁承业 恽榴红 《中国药物化学杂志》 CAS CSCD 1993年第2期79-84,共6页
本文首次用分子力学计算产物或过渡态分子内张力能来估算热力学或动力学,控制不对称合成反应生成的立体异构体的相对比例,并从热力学上推导了这一比例随温度变化公式,而且从实验上得到证明,在有机或药物化学最富有挑战性的领域——不对... 本文首次用分子力学计算产物或过渡态分子内张力能来估算热力学或动力学,控制不对称合成反应生成的立体异构体的相对比例,并从热力学上推导了这一比例随温度变化公式,而且从实验上得到证明,在有机或药物化学最富有挑战性的领域——不对称合成中具有重要的理论和实际意义。 展开更多
关键词 不对称合成 立体异构体 胆碱化合物 Α-氨基膦酸 热力学 分子力学
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Unexpected anterograde amnesia associated with Buscopan used as a predmedication for endocscopy
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作者 Hyuk Lee Hee Jung Son +2 位作者 Poong-Lyul Rhee Jae J Kim Jong Chul Rhee 《World Journal of Gastroenterology》 SCIE CAS CSCD 2007年第28期3895-3896,共2页
It has been known that peripheral adverse event is caused by peripheral antimuscarinic action, from hyoscine butylbromide (Buscopan; Boehringer Ingelheim, Germany) used as a premedication for endoscopy. However, sympt... It has been known that peripheral adverse event is caused by peripheral antimuscarinic action, from hyoscine butylbromide (Buscopan; Boehringer Ingelheim, Germany) used as a premedication for endoscopy. However, symptoms or signs associated with the central nervous system are rarely reported in the field of anesthesiology and peripartum labor. This central anticholinergic syndrome is likely caused by blockade of muscarinic cholinergic receptors in the central nervous system. There is no report on Buscopan-induced central anticholinergic syndrome in endoscopy room so far. Three middle-aged females unexpectedly suffered from anterograde amnesia after intramuscular injection of hyoscine butylbromide as an antispasmodic premedication for endoscopy at our endoscopy unit in the Health Promotion Center. 展开更多
关键词 ENDOSCOPY Hyoscine butylbromide Central anticholinergic syndrome AMNESIA
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Design, synthesis and biological evaluation of novel quinoline [4,3-b] chromene derivatives as AChE inhibitors through an efficient one-pot, four-component microwave-mediated reaction
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作者 Ming He Baohua Xie +3 位作者 Pei He Haxbing Zhou Shengtang Huang Chune Dong 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2018年第11期735-752,共18页
An efficient synthesis of chromeno[4,3-b]quinoline derivatives via one-pot,four-component reaction of 4-hydroxycoumarin, formaldehyde,cyclohexanedione,ammonium ceric nitrate under microwave irradiation was accomplishe... An efficient synthesis of chromeno[4,3-b]quinoline derivatives via one-pot,four-component reaction of 4-hydroxycoumarin, formaldehyde,cyclohexanedione,ammonium ceric nitrate under microwave irradiation was accomplished.The structures of these compounds were unambiguously confirmed by single crystal X-ray diffraction.Furthermore,the anti-AChE activities of these compounds in vitro were investigated at concentrations of 20μM and 50μM by using a standard Ellman's method.The relationship of inhibitory activities and structures of these chromeno [4,3-b]quinolines was also systematically studied.Of all the compounds investigated,4ag emerged as the most potent AChE inhibitor with IC50 values of 5.63μM,and it might be used as potent lead for the development anti-AChE agents.Moreover,molecular modelling was conducted to understand the optimal interaction of AChE with these types of compounds. 展开更多
关键词 Chromeno [4 3-b]quinoline Anti-AChE activities Molecular modelling Four-component reaction
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