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抗疟新药7351的合成 总被引:3,自引:0,他引:3
A new antimalarial drug 7351 (pyronaridine or malaridine), 2-methoxy-7-chloro10-[3', 5'-his- (pyrrolin-1-yl-methyl)-4'-hydroxyphenylamino]-benzo-[b]- 1,5-naphthy-ridine (Ⅱb), was synthesized. Experimental therapy and clinical trials showed that the results are satisfactory. No cross-resistance to chloroquine has been found in animals and in human cases. The drug could be given by oral, intramuscular injection or intravenous drip. It is specific for treatment of severe malaria cases. 相似文献
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作者等将对-氨基酚双Mannich碱的侧链与苯骈[g]喹啉、1,5-萘啶、吡啶骈[2,3-d]嘧啶,苯骈[c]吖啶、吡啶骈[2,3-c]吖啶以及吡啶骈[2,3-e]吖啶等杂环相连,合成了不同类型的杂环化合物V1~19。部分化合物经鼠疟Plasmodium berghei试验,发现化合物V1~3,8,10,12,18等具有杀灭红细胞内期裂殖体的作用。部分化合物用约氏原虫(P.yoelii)-斯氏按蚊(Anophelesstephensi)-鼠模型筛选,未见有明显作用。 相似文献
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我们曾将一例结核性胸腹壁慢性脓肿误诊为肝癌而进行了腹部手术,现报告如下。患者男,53岁,右上腹肋下有一核桃大小肿块,无痛,不发烧,食欲正常,消化良好,不厌油,不恶心呕吐,未觉消瘦和体重减轻,体力很 相似文献
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紫外线能杀灭多种致病微生物,因此,紫外线消毒法是临床上常用的物理消毒方法之一,笔于1991年1月~1992年12月对本院各科室所用的62支紫外线灯管强度进行了调查。结果发现紫外线灯管强度低于70μW/cm^2的达33.2%。还有的由于使用不当投有发挥应有的效应。本就如何正确使用紫外线灯予以探讨。 相似文献
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抗疟新药咯萘啶及其类似物的合成 总被引:8,自引:0,他引:8
作者等根据一些抗疟药的构效关系,合成了一种新化合物2-甲氧基-7-氯-10-[3′,5′-双(四氢吡咯次甲基)一4′-羟基苯胺基]苯骈[b]1,5-萘啶(Ⅰ),代号7351,定名咯萘啶。它对红内期裂殖体的作用显著,毒性低。之后,又合成了它的类似物Ⅱ,这些类似物大多数对鼠疟Plasmodiumberghei的红内期均具有不同程度的作用,其中Ⅱ1~6,9.10等的作用与Ⅰ相当。对子孢子诱发感染的鼠疟P.yoelii的作用以化合物Ⅰ、Ⅱ1,3,5,6,9,10,12,15等为最强,优于伯喹对照组。值得注意的是,这类化合物既对血液转种的鼠疟P.berghei具有显著的作用,同时对子孢子感染的鼠疟P.yoelii也具有显著的作用。 相似文献
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根据5-(对-氟苯氧基)-6-甲氧基-8-(4-氨基-1-甲基-丁氨基)喹啉(Ⅰ1)(表1)对猴疟原虫(Plasmodium cynomolgi)的作用略优于伯喹而毒性较低的报道,合成了化合物Ⅰ1(代号M7844),同时还合成了衍生物5-取代苯氧基-6-甲氧基-8-(4-取代氨基-1-甲基丁氨基)喹啉(Ⅰ3~17)(表1)以及其同分异构体5-取代苯氧基6-甲氧基-8-(5-取代氨基戊氨基)喹啉(Ⅱ13~28)(表2)。药理研究证明化合物Ⅰ1~7、Ⅰ16及Ⅱ18等对鼠疟P.yoelii均有不同程度的作用。化合物Ⅰ1(M7844)的毒性甚低,对小鼠的毒性比磷酸伯喹低20余倍,对家兔的溶血反应也明显低干伯喹。但在相同剂量下,对猴疟P.cynomolgi的作用不及伯喹。对鼠疟红前期的作用比伯喹低4~5倍。 相似文献
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A series of. analogues of 4-methyl-5-(p-fluorophenoxy)-primaquine have been prepared for evaluating of tissue schizonticidal actiyity of Plasmodium yoelii in mice. 2-Bromo-4-acetamino-5-nitroanisole was reacted with pfluorophenol in the presence of potassium hydroxide to give 2-(p-fluorophenoxy) 4-acetamino-5-nitroanisole, which was subsequently hydrolyzed to yield corresponding amino compound. Cyclization of the amino compound with methyl vinyl ketone afforded 4-methyl-5-(p-fluorophenoxy)-6-methoxy-8-nitroquinoline. This product was reduced by iron and acetic acid to give corresponding 8-aminoquinoline. The latter was condensed with bromoalkylphthalimides to yield 4-methyl-5-(pfluorophenoxy)-6-methony-8- (1-phthalimidoalkyl) aminoquinolines (Ⅳ1~Ⅳ7). These compounds were heated with hydrazine hydrate to form 4-methyl-5-(p-fluorophenoxy)-6-methoxy-8-(1-aminoalkyl)aminoquinolines(Ⅳ8~Ⅳ13), and 4-methyl-5-(p-fluorophenoxy) primaquine (Ⅱ).Compound Ⅱ synthesized was radical curative at 10 mg/kg×1, while the analogues Ⅳ9 and Ⅳ10 were radical curative at 100 mg/kg×1 against P. yoelii in mice. 相似文献