共查询到20条相似文献,搜索用时 15 毫秒
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S. V. Ukhov B. Ya. Syropyatov V. V. Novikova V. A. Balabash A. S. Shustov T. F. Odegova 《Pharmaceutical Chemistry Journal》2011,45(4):228-230
Interaction of 2-hydroxynaphthaline-1-carbaldehyde with cyanoacetic acid arylamides was used to synthesize substituted 2-iminobenzo[f]coumarin-3-carboxylic acid amides. Heating of substituted 2-iminobenzo[f]coumarin-3-carboxylic acid amides with acetic anhydride led to the synthesis of acetyl derivatives of this acid. The anticoagulant and antimicrobial activities of these compounds were studied. 相似文献
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摘 要: 目的 设计并合成&;#61538;-分泌酶(BACE1)的小分子抑制剂。方法 基于BACE1的晶体结构及其配体的关键结构特征,设计并合成新结构的BACE1配体。结果与结论 合成了26个酒石酸衍生物。筛选结果表明,部分化合物对BACE1有一定的抑制作用。 相似文献
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Synthesis of some substituted quinazolinediones as potential inhibitors of smooth muscle contraction
3-Substituted 2,4(1H,3H)-quinazolinediones were prepared from the corresponding N-substituted 2-aminobenzamides by treatment with ethyl chloroformate and KOH in ethanol. Also, a series of 3-substituted and 1-methyl-3-substituted 2,4(1H,3H)-quinazolinediones were synthesized by the reaction of 1-methyl-1,4-dihydro- and 1,4-dihydro-2,4-dioxo-3(2H)-quinazolineacetic acid with the corresponding N-substituted piperazines. The 13C NMR spectra and mass spectra of the compounds were measured and signals were assigned. Some of the compounds showed inhibitory action on contractile function of smooth muscle. 相似文献
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Altmann E Renaud J Green J Farley D Cutting B Jahnke W 《Journal of medicinal chemistry》2002,45(12):2352-2354
A series of N(alpha)-benzyloxycarbonyl- and N(alpha)-acyl-L-leucine(2-phenylaminoethyl)amide derivatives were prepared and evaluated for their inhibitory activity against rabbit and human cysteine proteases cathepsins K, L, and S. These data indicate that N(alpha)-acyl-alpha-amino acid-(arylaminoethyl)amides represent a new class of selective non-covalent inhibitors of cathepsin K. Compounds 4b, 4e, and 4g exhibit high potency toward rabbit and human cathepsin K (IC(50) < 0.006 microM) and are characterized by an excellent selectivity profile vs human cathepsins L and S. 相似文献
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S Konno M Sagi K Wada F Shiga H Yamanaka 《Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan》1992,112(10):768-772
A series of 6-alkylaminopyridazine-3-carboxylic acid derivatives was tested for dopamine beta-hydroxylase inhibitory activity in vitro according to the method of Kruse et al. Methyl 6-alkylaminopyridazine-3-carboxylates (4) were synthesized through the reaction of methyl 6-chloropyridazine-3-carboxylate (1) with ammonia followed by the condensation with primary amines, and by the methanolysis of the resulting 6-alkylaminopyridazine-3-carboxamides (3) in methanol in the presence of boron trifluoride etherate. Among tested compounds, 6-benzylaminopyridazine-3-carboxylic acid was found to have the most potent inhibitory activity, which was in the same level of the activity of fusaric acid. 相似文献
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1-甲基-3-正丙基吡唑-5-甲酸乙酯的合成 总被引:1,自引:0,他引:1
目的:合成标题化合物,并进行工艺改进。方法:以2-戊酮和草酸二乙酯为原料,经三步反应合成了产物。结果:反应的总收率为47.7%。合成的各步产品经元素分析、红外和核磁共振光谱确证。结论:改进的工艺具有反应温度低、时间短等优点,并提高了收率。 相似文献
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In search of novel purine antimetabolites, a series of 8-substituted methylxanthine derivatives was prepared in order to explore their in vitro anticancer, anti-HIV-1 and antimicrobial activities. The target compounds include: 8-[(3-substituted-4-oxo-thiazolidin-2-ylidene)hydrazino]-1,3-dimethyl (or 1,3,7-trimethyl)-3,7-dihydropurine-2,6-diones 5a-e, 8-[(3,4-disubstituted 2,3-dihydrothiazol-2-ylidene)hydrazino]-1,3,7-trimethyl-3,7-dihydropurine-2,6-diones 6a-d and 8-(5-amino-3-arylpyrazol-1-yl)-1,3-dimethyl- (or 1,3,7-trimethyl)-3,7-dihydropurine-2,6-diones 7a-g. The in vitro anticancer results revealed that compound 5d exhibited a super sensitivity profile towards leukemia K-562 with a GI(50) value of <0.01 microM. Compound 7c showed significant activity against colon cancer HCT-15 and renal cancer CAKI-1 (GI(50) values of 0.47 and 0.78 microM, respectively). Compound 7a displayed high activity against colon cancer HCT-15 (GI(50 )= 0.8 microM). The anti-HIV-1 results indicated that compound 6b displayed a good reduction of viral cytopathic effect (56.69%). The antimicrobial results showed that compound 5a was four times more active than ampicillin against P. aerugenosa (MIC =or< 25 microg/mL), compound 5b had twice the activity of ampicillin, while compounds 5d, 7c and 7f were equipotent to ampicillin. On the other hand, compound 7a was equipotent to ampicillin against P. vulgaris (MIC = 50 microg/mL). 相似文献
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Mao Zhang Xiang Lu Hong-Jia Zhang Na Li Yu Xiao Hai-Liang Zhu Yong-Hao Ye 《Medicinal chemistry research》2013,22(2):986-994
A series of derivatives of cinnamic amide (compounds 2a–2v) were synthesized and evaluated for antiproliferative activities against the human breast cancer cell line MCF-7- and EGFR-inhibitory activities. The structures of compounds 2b and 2i were determined by single-crystal X-ray diffraction analysis. Compounds 2f and 2j showed moderate EGFR inhibitory activity with IC50 values of 5.16 and 7.37 μM, respectively. Docking simulation of compound 2f was carried out to illustrate the binding mode of the molecule into the EGFR active site. Structure–activity relationship analysis found that the N-phenyl rings are required for enhancing the activities. 相似文献