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analogues
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  类似物
    Studies on the Synthesis of New Taxol Analogues
    新型紫杉醇类似物的合成研究
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    Design, Synthesis, Antitumor Mechanism and Structure-Activity Relationships of WB852 Analogues
    WB852类似物的设计、合成及其抗癌作用机理和构效关系研究
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    NEUROPHARMACOLOGICAL ACTIONS OF SOME 5-HYDROXYTRYPTAMINE ANALOGUES
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    SYNTHESIS OF ACTINOMYCIN ANALOGUES——Ⅳ. SYNTHESIS OF 2-AMINO-4, 6-DIMETHYLPHENOXAZONE-(3)-1, 9-BIS-PEPTIDES
    放线菌素类似物的合成Ⅳ——2-氨基-4,6-二甲基吩(口恶)嗪酮-(3)-1,9-双多肽的合成
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    SYNTHESIS OF MEXILETINE ANALOGUES
    “慢心率”(mexiletine)类似物的合成
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    Pharmacokinetics Study on the Analogues of M-Nifedipine
    间硝苯地平同系物的代谢动力学研究
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    TUMOUR CHEMOTHERAPY SYNTHESES OF N-ACETYL-N-{3-[BIS-(β-CHLOROETHYL)-AMINO]-6-METHYL-PHENYL}-GLYCINE AND ITS DEMETHYL ANALOGUES
    肿瘤的化学治疗ⅩⅩⅫ.N-乙酰基-N-{3-[双-(β-氯乙基)-氨基]-6-甲基(或氢)-苯基}-甘氨酸的合成
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    TUMOUR CHEMOTHERAPHY ⅩⅩⅩⅧ SYNTHESIS OF ANALOGUES OF CHLORAMPHENICOL
    肿瘤的化学治疗——ⅩⅩⅩⅧ.氯霉素同型物的合成
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    SYNTHESIS OF ~(35)S-LABELLED O-ETHYL-S-2-DIISOPROPYLAMINO-ETHYL-METHYLPHOSPHONOTHIOATE (VX) AND ITS ANALOGUES
    ~(35)S-硫代甲膦酸(O-烷基-S-2-二烷基氨基乙基)酯及其季铵盐的合成
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    STUDIES ON ANTIMALARIALS.Ⅺ.SYNTHESIS AND ANTIMALARIAL EFFECTS OF 4-METHYL-5-SUBSTITUTED PHENOXY PRIMAQUINE ANALOGUES
    抗疟药的研究 Ⅺ.4-甲基-5取代苯氧基伯喹的合成及其抗疟作用
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  analogues
A number of q,t-analogues of this fact were conjectured in [10]; the present paper proves most of those conjectures, as well as some new identities suggested by the proof technique.
      
Higher dimensional analogues of these results, which apply to functions $f\in L^p[-R,R]^d$ and $C^{m-2-k}[-R,R]^d,$ are proven.
      
SYNTHESIS OF THE RIGID ANALOGUES OF AN SSRI BENZENEPROPANAMINE
      
Synthesis and Structure-Activity Relationships of Vasicine Analogues as Bronchodilatory Agents
      
The series of vasicine (1) analogues, an alkaloid from Adhatoda vasica Nees., were synthesized with changes in A, B or C rings.
      
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The fact that 2-alkoxy-5-aminopyridines(Ⅰ)and 2-alkoxy-6-aminobenzothiazole(Ⅱ)possess high tuberculostatic activities in vitro as well as in experimental animals led us to prepare a num- ber of analogous compounds belonging to quinoline series,namely,2-alkoxy(n-propoxy,or n- butoxy)-6-aminoquinoline(Ⅲe or Ⅲa)and its structural isomers,2-butoxy-5-(or 7-,or 8-)- aminoquinoline(Ⅲb,Ⅲc,or Ⅲd);and 2-butoxy-6-acetamino-(or dichloroacetamino-,or dimethy- lamino)-quinoline(Ⅳa,or Ⅳb,or Ⅳc)for the purpose of testing their...

The fact that 2-alkoxy-5-aminopyridines(Ⅰ)and 2-alkoxy-6-aminobenzothiazole(Ⅱ)possess high tuberculostatic activities in vitro as well as in experimental animals led us to prepare a num- ber of analogous compounds belonging to quinoline series,namely,2-alkoxy(n-propoxy,or n- butoxy)-6-aminoquinoline(Ⅲe or Ⅲa)and its structural isomers,2-butoxy-5-(or 7-,or 8-)- aminoquinoline(Ⅲb,Ⅲc,or Ⅲd);and 2-butoxy-6-acetamino-(or dichloroacetamino-,or dimethy- lamino)-quinoline(Ⅳa,or Ⅳb,or Ⅳc)for the purpose of testing their antimycobacterial ac- tivities,and also of studying the relationships between antibacterial activity and chemical structure. Besides,several 2-alkoxy-6-aminocinchoninic acid hydrazides(Ⅳa,Ⅳb,Ⅳc,Ⅳd,Ⅳe),were also prepared.As can be seen from the formula,there is an additional—CONHNH_2 group present in the molecule as compared with Ⅲa and its alkoxy analogues. The results of antimycobacterial activities against mycobacterium 607 and smegmatis activities are listed in tables 1—3. Ⅲa possesses 1/2—1/4 activity against mycobact.607 as compared with that of INH,but is comparable to the latter in the case of antismegmatis activity.Ⅲb,Ⅲc and Ⅲd possess the similar order of activity as Ⅲa.2-Hydroxy-6-aminoquinoline and also all the corresponding nitro- compounds of Ⅲa,Ⅲb,Ⅲc,Ⅲd and Ⅲe are of no significant activity.The acylated and methylated compounds of Ⅲa are also with much less activities,p-Amino-N-carbobutoxyaniline (Ⅴ)which was thought to be an open-ring compound of Ⅲa is also inactive.These facts show that the free amino and alkoxyl groups attached to aromatic structure are necessary for the exhibition of antimycobacterial activity.As to the position of the amino group attached to the benzene moiety of quinoline nucleus seems without practical influence.The introduction of a carbohydrazino group to the 4-position of Ⅲa or of its alkoxyl analogues is unfavorable to the in vitro antimycobacterial activity. The methods of preparation of compounds of type Ⅲ were by treating at first the 2-chloro- nitroquinolines(Ⅶ)with an appropriate sodium alcoholate to form 2-alkoxy-nitroquinolines (Ⅷ),and then the latter reduced by stannous chloride to give the required products(Ⅲ). The synthesis of the compounds of type Ⅵ was to begin with 2-chloro-6-nitrocinchoninic acid chloride(Ⅸ),which by treating with methyl or ethyl alcohol to give the corresponding methyl or ethyl esters(Ⅹ).The latter were then reacted with the appropriate sodium alcoholates to afford 2-alkoxy-6-nitrocinchoninic acid methyl or ethyl esters(Ⅺ),which were then catalytically reduced in the presence of Pd-C to give the corresponding amino-compounds (ⅩⅢ).The desired pro- ducts(Ⅵ)were obtained by treating the latter with hydrazine hydrate.Ⅺ directly reacted with hydrazine hydrate to give Ⅻ. Solvents of crystallization,melting points,yields of the compounds synthesized in this inves- tigation are summarized in table Ⅳ.

1.本文叙述了2-烷氧基-6-(或5-,或7-或8-)氨基喹啉,以及2-正丁氧基-6-乙酰(或二氯乙酰,或二甲)氨基喹啉的合成.2.合成了2-烷氧(甲氧,或乙氧,或正丙氧,或正丁氧)基-6-氨基辛可宁酸酰肼.3.将上述各产物及其中间体均进行了对结核分枝杆菌607及恥垢杆菌的体外抑制作用.结果表示Ⅲ类型化合物在体外的抗结核杆菌作用仅与联在芳香环上的烷氧基及伯氨基有关,而氨基在喹啉环的苯环部分上的位置则无关.4.加入一个羰肼基于Ⅲa 及其烷氧基同系物的4-位上对体外抗结核杆菌作用不利.

In view of some analogues of chloramphenicol show more or less in vitro activity towards quite a few species of tumour cells,the authours have examined the in vitro anti-Ehrlich ascites activity of 5 compounds prepared by one of us and Par before,namely,α-dichloroacetamido- (or acetamido)-β-hydroxy-p-nitro-o-hyrdroxy-(or methoxy)-propiophenone(Ⅰ,Ⅱ,Ⅲ),and α-dichloro- acetamido-β-hydroxy-p-amino-o-hydroxy-propiophenone(IV, V).The results(see Tab. 1)showed that the compounds carrying a nitro group in the...

In view of some analogues of chloramphenicol show more or less in vitro activity towards quite a few species of tumour cells,the authours have examined the in vitro anti-Ehrlich ascites activity of 5 compounds prepared by one of us and Par before,namely,α-dichloroacetamido- (or acetamido)-β-hydroxy-p-nitro-o-hyrdroxy-(or methoxy)-propiophenone(Ⅰ,Ⅱ,Ⅲ),and α-dichloro- acetamido-β-hydroxy-p-amino-o-hydroxy-propiophenone(IV, V).The results(see Tab. 1)showed that the compounds carrying a nitro group in the benzene ring possessed invariably higher activity as compared with their corresponding amino analogues.Therefore,it appears that the nitro group attached to benzene ring plays somewhat important role in producing the in vitro anti-Ehrlich ascites activity. These facts led us to prepare some arylaliphatic nitroalcohols(Ⅶ,Ⅸ,Ⅹ,Ⅺ)and some derivatives of β-nitrostyrenes (Ⅻ, ⅩⅣ,ⅩⅤ,ⅩⅥ,ⅩⅦ,ⅩⅧ,ⅩⅨ,ⅩⅩ) for the purpose of examining their anti-Ehrlich ascites activity.The results(see Tab.2)showed that the nitro group attached to saturated aliphatic carbon atom has no obvious influence in enhancing the anti-tumour activity,in some cases even with counter effect,but that which attached to unsaturated aliphatic carbon atom,as in the case of a series of β-nitrostyrene derivatives,did show higher activity.Therefore, the phenomenon is in harmony with the result described for I,II in the foregoing paragraph,that is,nitro group attached to unsaturated carbon atom is equivalent to that attached to benzene ring. 1-Phenyl-4-nitrobutadiene(ⅩⅥ),in which the nitro group being in the vinylogous position of β-nitrostyrene,also possessed considerable activity.The groups,except that with greater molar volume,substituted in'the benzene nucleus of β-nitrostyrene appear to have no significant influ- ence. The m.ps.of the compounds prepared are recorded in Tab.2.

1.試驗了α-二氯乙酰胺(或乙酰胺基)-β-羥基-对-硝基-邻羥基(或甲氧基)苯丙酮及其相当的氨基化合物的体外抗艾氏腹水瘤細胞的作用,表示硝基对产生活力有影响。2.合成了若干芳香脂肪硝基化合物及β-硝基苯乙烯类化合物,并試驗了該項化合物的体外抗艾氏腹水瘤細胞的活力。3.从活力与化学結构的关系看,脂肪族飽和碳原子上的硝基对产生抗瘤細胞活力无影响,而硝基連在不飽和碳原子上时对活力的增強有很大关系。故一系列的β-硝基苯乙烯类化合物均有相当好的抗肿瘤細胞作用。至于苯乙烯环上的取代基則关系不大,除非取代的基团体积較大,活力也减小。

The antimonial chelates of ethylenediaminetetraacetic acid (Ⅱ, EDTA), propylenediaminetetraacetic acid (Ⅲ, PDTA) and nitrilotriacetic acid (Ⅳ, NTA) were reported to exhibit inhibitory activities on tumours, but the antimonial chelates of cyclohexane-1,2-diaminetetraacetic acid (Ⅰ) and β-hydroxyethylaminediacetic acid (Ⅴ) were found to be non-effective on the tumour growth in vivo. The relative stabilities of the amino polycarboxylic acid chelates of antimony were observed by Chue to be: Ⅰ>Ⅱ>Ⅲ>Ⅳ>Ⅴ. In this connection...

The antimonial chelates of ethylenediaminetetraacetic acid (Ⅱ, EDTA), propylenediaminetetraacetic acid (Ⅲ, PDTA) and nitrilotriacetic acid (Ⅳ, NTA) were reported to exhibit inhibitory activities on tumours, but the antimonial chelates of cyclohexane-1,2-diaminetetraacetic acid (Ⅰ) and β-hydroxyethylaminediacetic acid (Ⅴ) were found to be non-effective on the tumour growth in vivo. The relative stabilities of the amino polycarboxylic acid chelates of antimony were observed by Chue to be: Ⅰ>Ⅱ>Ⅲ>Ⅳ>Ⅴ. In this connection it was interesting to note that the antitumour activity seemed to be associated only with moderately stable chelates with antimony such as formed from PDTA-Sb and NTA-Sb. Since the introduction of nonchelating substituents in the chelating ligand might alter the basicity of the electron donor atom, or might prevent the most favourable metal-ligand orientation, it would be advisable to prepare the amino polycarboxylic acids (Ⅵ a—f), presumably having lower stability constant, related to nitrilotriacetic acid. The analogues of NTA (Ⅵ a m. p. 200—1℃; Ⅵ b m. p. 138—140℃; Ⅵ c m. p. 171—173℃; Ⅵ d m. p. 186—188℃; Ⅵ e m. p. 184—185℃; Ⅵ f m. p. 146—148℃) were prepared by the reaction of monochloroacetic acid with the dl-amino acids (alanine, isobutyric amino acid, α-aminobutyric acid, leucine, β-phenylalanine, aspartic acid, respectively). The aqueous reaction mixtures were passed through Zerolite 225-SO_3H to remove the sodium ion. The authors found that the use of resin was more convenient than the conventional method of acidification with inorganic acid. Difficulties were encountered in obtaining the amino polycarboxylic acids, Ⅵ, in crystalline. form in the presence of inorganic acids. In the case of Ⅵ f, the reaction mixture was passed through Amberlite IRA-401-OH to remove chloride ion, then through Zerolite 225-SO_3H to remove sodium ion. If the chloride ion was not removed, probably deamination took place (in the presence of hydrochloric acid) upon evaporation, and the reaction product was found not to be Ⅵ f. The amino polycarboxylic acids (Ⅵ a, c, d, e) on treatment with freshly precipitated antimonous acid or butyl antimonite according to Chue-Kyi's procedure, gave the corresponding antimonial chelates in which each antimonial atom combined with two molecules of chelating agents. Compound Ⅵ f failed to give a satisfactory chelate. Owing to low stability these antimonial chelates tend to decompose on recrystallization by conventional procedure. They were purified, as follows: the crude products were dissolved in large amount of warm water, the impurity was separated by filtration, and the filtrate was evaporated to dryness at low temperature under reduced pressure. Several repetitions of this procedure might be needed to give the analytical sample. Preliminary pharmacological tests revealed that the antimonial chelates of Ⅵ a (10 mg/kg), Ⅵ c (15 mg/kg) and Ⅵ e (20 mg/kg) inhibited the growth of Ehrlich ascites carcinoma of mice, but possessed no inhibitory action on sarcoma 180.

一氯乙酸分别与丙氨酸、异丁氨酸、a-氨基丁酸、亮氨酸、天门多氨酸、苯丙氨酸作用,制成一系列与氨三乙酸类似的胺羧络合剂,并借离子交换树脂除去溶液中的无机盐而提纯。化合物VIa,c,d,e与亚锑酸或亚锑酸丁酯反应所形成的锑螯合物,其结合比例亦如 NTA,即一原子的锑和二分子的络合剂所形成。但螯合能力,从化学反应上推测,则较NTA为弱。上述锑螫合物系供肿瘤动物实验之用。初步报告,应用VIa-Sb,VIc-Sb及VIe-Sb分别为10,15及20毫克/公斤剂量时,能抑制小白鼠Ehrlich腹水瘤的生长(其抑制率分别为36%,65%及64%)。对肉瘤180则无抑制作用。

 
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