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1.
A series of bis(2,4-diamino-quinazol-6-yl-substituted aminomethyl) aromatic derivatives were synthesized. Compounds Ⅱ1~5 were synthesized by two ways. In the first, 2,4,6-triaminoquinazoline was condensed with the corresponding aryl dialdehydes to form Schiff bases which were reduced with sodium borohydride; the second used a new method in which 2,4,6-triaminoquinazoline was directly condensed with the corresponding aralkyl dihalides to afford the same products. The derivatives Ⅱ6~16 were prepared by formylation, nitrosation or methylation respectively.The inhibition activities of the title compounds on dihydrofolate reductase in rat liver were assayed. The activities of formylated or nitrosated products were 6-9 times, and of methylated products were twofold as active as that of the parent compounds. Ⅱ6, Ⅱ9, Ⅱ10 and Ⅱ14 were nearly as potent as pyrimethamine. Primary antimalarial screening in mice showed that no one possessed significant activity. 相似文献
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2,4-Diamino-6-substituted amino sulfonyl quinazolines generally were prepared by refluxing 2,4-diamino-6-chloro-sulfonylquinazoline sulfate with suitable amines in dilute ethanol. For 2,4-diamino-6-(2-pyridy) amino sulfonyl quinazoline, it was prepared in dry pyridine. Compounds Ⅰ2, Ⅰ9 and Ⅰ10 were shown to be more active against chloroquine resistant strain of P. berghei than sensitive strain. Compounds Ⅰ2, Ⅰ12 and Ⅰ13 showed prophylactic action against P. yoelii. 相似文献
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Ten 4-nitrodiphenylether-4′-thiocarbamides were synthesized from 4-nitro-4′-thiocyanodiphenylether and corresponding amines. Preliminary screening data in table 1 showed that most of them exhibited insignificant or low activity against schistosoma japonicnm in mice, while V9 with a diethyl substituted nitrogen in thiocarbamide structure was found to possess antischistosomal activity as high as that of nithiocyamine (Amoscanatec9333 GO/COP 4540). 相似文献
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青蒿素类似物的研究 Ⅶ.双(二氢青蒿素)醚和双(二氢脱氧青蒿素)醚类化合物的合成 总被引:1,自引:0,他引:1
Some ethers, of bis(dihydroqinghaosu) Ⅲ and bis(dihydrodeoxyqinghaosu) Ⅳ were prepared in order to study the structure-activity relationships and to search for new antimalarials. Compounds Ⅲ were sythesized by condensation of glycol with two moles of dihydroqinghaosu using boron trifluoride etherate as catalyst. Compounds Ⅳ were prepared from ethers of bis (dihydroqinghaosu) by reduction with zinc and acetic acid.The bis-ethers were evaluated against chloroquine-resistant strain of plasmodium berghei in mice. Compounds Ⅲ were less potent than methyl-dihydroqinghaosu (Ⅰ) and compounds Ⅳ were inactive. 相似文献
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According to the principle of isosterism the-CH2-group of 5-(substituted benzyl)-2, 4-diaminopyrimidine was modified by—S—and—Se—and some 5-(substituted phenyl)thio-2, 4-diaminopyrimidines and 5-(substituted phenyl)seleno-2,4-diaminopyrimidines were synthesized. Their inhibitory activities on L. casei and chicken liver dihydrofolate reductase were determined. Preliminary data showed that the inhibitory activities of these compounds were less than those of the corresponding 5-(substituted benzyl)-2, 4-diaminopyrimidines. Their selectivities are also decreased. 相似文献
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Synthesis of 35 new compounds of α-chloro-β-(5-nitro-2-furyl) acrylamides and 5-[α-chloro-β-(5-nitro-2-furyl ) vinyl]-oxadiazoles by known methods are reported. In preliminary test in mice 10 compounds were found to possess pronounced activity against Schistosomiasis japonica. Among these Ⅰ12, Ⅰ13, Ⅰ14, Ⅰ20, Ⅱ1 and Ⅱ8 were shown to be the most effective. 相似文献
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In order to search for effective antimyocardial ischemic agents, fourteen new 3 4-[(3-alkylamino-2-hydroxy)propoxy] phenyl(benzyl)]-substituted 4(3H)-quin zolinones (Ⅱ) were synthesized. Substituted o-aminobenzoic acids used as the starting materials were allowed to react with acetic anhydride and then p-aminophenol (method A), or with N- (4- hydroxyphenyl)formamide (method B), or with thionyl chloride and then N - (4 - hydroxybenzyl) formamide (methode C) to form 3-[(4-hydroxyphenyl(benzyl)]-substituted 4(3H)-quinazolinones (Ⅲ). The intermediate Ⅲ reacted with epichiorohydrin to form the epoxides (Ⅳ). The reaction of Ⅳ with an excess of isopropylamine or tert-butylamine in boiling chloroform gave the desired products. Of all the compounds synthesized, Compounds Ⅱ3~5 and Ⅱ13 were found to increase the tolerance of mice to hypoxia. Further evaluation is in progress. 相似文献
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Synthesis of p-chlorophenylpropiolylamides and itsreaction produets with hydrazine hydrate were studied. It was found that the reaction products varied with the different Substituent groups in the amidel When the substituent group was isopropyl or sec-butyl group, p-chloro-β-hydrazino-cinnamamides (Ⅱ) were obtained. Under similar reaction conditions, when the substituent, group was n-propyl, n-butyl or diethyl group, cyclization reaction occurred and the reaction product was 3-(p-chlorophenyl)-pyrazol-5-one (Ⅲ). All the compounds were tested in mice for anticonvulsant activity. Prelimary data showed that p-chlorophenyl-propiolyl-sec-butylamide (I4) and p-chlorophenyl-propiolyl-n-propylamide (I1) exhibited moderate anticonvulsant activity. The ED50 was 54.5(34.4~86.4), and 56.1(31.6~99.6) mg/kg respectively. The compounds of p-chloro-β-hydrazino-cinnamamide (Ⅱ)and 3-(p-chlorophenyl)-pyrazol-5-one (Ⅲ) showed no significant effect on antieonvulsant activity. p-Chloro-cinnamoyl-hydrazide (Ⅳ) provided good anticonvulsant activity. 相似文献
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2-Imino-3-(β-hydroxyphenethyl)thiazolidine showed hypotensive activity. In order to find more active derivatives, a series of compounds has been synthesized.In preliminary screening tests, Compounds (Ⅱ-2) and (Ⅳ-1) showed considerable hypotensive effect. 相似文献
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Seventeen compounds having the structure of 2,3-diacetoxy-1,4-bis(3′,5′- dioxo-N4′-substituted piperazinyl methyl)benzene were designed and synthesized based on chelation hypothesis. Their antitumor activities on P388 cells,Hep cells and SGC 7901 cells in vitro were tested. Preliminary results showed that compound 4e has potent antitumor effect against P388 cells and.Hep cells in vitro. 相似文献
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本文报道了2,4-二氨基-6-N1,N2-二取代肼基-喹唑啉类衍生物的合成及其抗疟活性的研究。这类化合物的合成是以2,4-二氨基6-取代苄基氨基-喹唑啉为原料经亚硝化、还原成为2,4-二氨基6-(N1-取代苄基)—肼基喹唑啉,再与相应的醛缩合而成。此类化合物经伯氏鼠疟原虫抑制性治疗初筛表明有少数具有一定的效果。有11个化合物经约氏鼠疟原虫—斯氏按蚊系统病因性初筛有效。其中化合物Ⅱ1,7,8,11,15和Ⅲ1口服2.5mg/kg,连续3天,可使受试小鼠全部得到保护。 相似文献
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2,4-二氨基喹唑啉类化合物为叶酸拮抗剂,对多种动物疟原虫有较好的作用。Elsla-ger等报道2,4-二氨基-6-[(间-三氟甲苯基)硫代]喹唑啉(Ⅰ)对鸡疟(Plasmodiumgallinaceum)子孢子和鼠疟(Plrsmodium berghei)滋养体均有较好的杀灭作用,对乙胺嘧啶敏感的Oak Knoll株和抗乙胺嘧啶的马来亚Camp株感染的枭猴也有治愈作用。鉴于三氟甲基在抗疟药中的独特作用和喹唑啉亚硫酰、硫酰类化合物(Ⅱ)对鼠疟有较好作用的 相似文献
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本文报道2,4-二哌啶(或吡咯啶)基-6-取代氨基喹唑啉衍生物的合成及其抗疟作用。该类化合物经伯氏鼠疟原虫(Plasmodium berghei)抑制性治疗和约氏鼠疟原虫(P.yoelii)病因性预防筛选,发现有16个化合物对感染约氏鼠疟原虫的小鼠有病因性预防作用,其中以Ⅵ11,Ⅷ1,Ⅸ2及Ⅸ4四个化合物效果最好,每天口服2.5 mg/kg,连续三天,可使小鼠得到完全保护。此类化合物的合成,是以2,4-二氯-6-硝基喹唑啉与哌啶或吡咯啶缩合,经还原得2,4-二哌啶(或吡咯啶)基-6-氨基喹唑啉,然后与相应的取代苯甲醛缩合成席夫氏碱,再经还原和亚硝化而制得。 相似文献
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Twenty-five compounds of N3-amino substituted quinazolone-4 have been synthesized and screened for activities against Plasmodium berghei and P yoelii in mice. No activity was found in these compounds. 相似文献