共查询到17条相似文献,搜索用时 187 毫秒
1.
Xing Zhou LI Xian Ping DAI Jun Hai XIAO Song LI* Beijing Institute of Pharmacology & Toxicology Beijing School of pharmaceutical Engineering Shenyang Pharmaceutical University Shengyang 《中国化学快报》2005,16(9):1137-1139
For discovering novel small molecule inhibitors of transforming growth factor-β1(TGF-β1)type-I receptor(ALK5),we designed1,3,5-triaryl-4-hydroxyl-4,5-dihydro-1H-pyrazole(1)as target compound,mimic the structure of SB-431542which is a2-pyridyl substituted triarylimiazole inhibitor of ALK51.Racemic compound1showed moderate ALK5inhibitory activity in luciferase reporter assays[inhibition(%control):0.1umol/L8.79%;1umol/L19.05%].To investigate the influence of the absolute configuration of… 相似文献
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De Jiang LI He Qing FU 《中国化学快报》2006,17(5):625-627
1, 3, 4-Oxadiazoline derivatives are found to possess significant biological activities such as antifungal1, insecticidal2, CNS depressant3-5, anticonvulsant effects and plant growth accelerator. They are highly important heterocycles, and have been used … 相似文献
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Synthesis, Crystal Structure and Bioactivities of 1-(4-Chlorophenyl)-3- [ 5-(pyrid-4-yl)- 1,3,4-thiadiazol-2-yl] urea 总被引:1,自引:0,他引:1
The title compound 1-(4-chlorophenyl)-3-[5-(pyrid-4-yl)-1,3,4-thiadiazol-2-yl]urea (C14H10ClN5OS, Mr = 331.79) has been synthesized by the reaction of 2-amino-5-(pyrid-4-yl)- 1,3,4-thiadiazole with 4-chlorobenzoyl azide, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to triclinic system, space group P with a = 5.8550(8), b = 7.5668(10), c = 16.416(2) , α = 78.364(2), β = 81.204(2), γ = 84.749(2)°, V = 702.58(16) 3, Z = 2, Dc = 1.568 g/cm3, μ = 0.429 mm-1, F(000) = 340, the final R = 0.0442 and wR = 0.1092 for 2001 observed reflections (I > 2σ(I)). X-ray diffraction analysis reveals that the title molecule is nearly planar. In the crystal structure, the molecules are linked by strong intermolecular N-H…N hydrogen bonds together with weak nonclassical intermolecular (C-H…Y, Y = N, O and Cl) hydrogen bonds and stacked through π-π interactions. The preliminary bioassay shows that the title compound exhibits good fungicidal activities against Rhizoctonia solani, Botrytis cinerea and Dothiorella gregaria. 相似文献
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1 INTRODUCTION 1,3,4-Thiadiazole derivatives represent an interes- ting class of compounds possessing broad spectrum biological activities[1~4]. Aroyl ureas are known to exhibit diverse biological effects, such as insecticidal, fungicidal, herbicidal and plant growth regulating activities[5~8]. Therefore, it is worthwhile to investi- gate the compounds incorporating both 1,3,4-thiadia- zole nucleus and aroyl urea group. In the previous paper[9], a series of aroyl ureas containing 1,3,4-t… 相似文献
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1INTRODUCTIONManypyrazolederivativeshavebeenreportedtoshowvariousbiologicalactivitiestobeusedasbactericide[1],fungicide[2],herbicide[3],insecticide[4]andvirucide[5]agents.Inaddition,4-thiazolidinoneplaysavitalroleowingtoitswiderangeofbiologi-calactivities… 相似文献
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De Jiang LI He Qing FU 《中国化学快报》2006,17(6):755-756
s-Triazolo[3, 4-b]-[1, 3, 4]thiadiazole derivatives have been paid attractive attention due to their significantly biological activities1-5, including antibacterial, antifungal, anticancer, relaxing vascular activities. They are highly important heterocyc… 相似文献
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JiuYuLIU HuiYuanGUO 《中国化学快报》2004,15(5):535-538
New quinolone derivatives of 7-[(2S, 4R)-2-aminomethyl-4-hydroxypyrrolidin-l-yl] quinolone-3-carboxylic acids were synthesized by condensation of 7-halo substituted quinolone-3-carboxylic acids with (2S, 4R)-2-aminomethyl-4-hydroxypyrrolidine. These compounds were characterized by FAB-MS and IH NMR. 相似文献
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CHEN Xiao-Bao LI Ke SHI De-Qing 《结构化学》2008,27(11):1389-1392
The crystal structure of the title compound (C12H10ClN7OS, Mr= 335.78) has been determined by single-crystal X-ray diffraction. The crystal is of triclinic, space group Pi with a = 8.4093(11), b = 9.4430(12), c = 11.1454(14) A, α = 95.508(2), β = 111.366(2), γ = 115.259(2)°, V = 711.42(16) A3, Z = 2, Dc = 1.568 g/cm3, F(000) = 344, μ(MoKα) = 0.428 mm-1, the final R = 0.0476 and wR = 0.1243 for 2353 observed reflections (I 〉 2o(/)). The dihedral angles between the pyridine and triazole, thiazole and triazole, and pyridine and thiazole rings are 69.2(1), 9.2(1) and 72.7(1)°, respectively. Intramolecular C(8)--H(8B)...O(1) and N(5)-H(5A)..-N(4) as well as intermolecular C(5)-H(5)...S(1), C(3)-H(3).,.N(6) and N(5)-H(5A)...N(1) hydrogen bonds together with weak C-H...Ir hydrogen-bonding and π-π stacking interactions contribute to the stability of the structure. There is also evidence for significant electron delocalization in the triazolyl system. 相似文献
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WAN Jun LI Chun-li LI Xue-mei ZHANG Shu-sheng 《高等学校化学研究》2006,22(4):465-467
The title compound was synthesized and characterized by IR, ^1H NMR, elemental analysis and single crystal X-ray diffraction analysis. Its biological activities were also tested. The results show that the title compound reveals inhibiting activities towards wheat gibberellin, apple ringspot, tomato early blight, peanut cercospora arachidicola and stem wilt of asparagus. 相似文献
11.
超声辐射下合成1-[(未)取代苯酰基-3-[5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑-2-基]-硫脲 总被引:2,自引:0,他引:2
1-苯基-3-甲基-5-氯吡唑-4-甲酸与氨基硫脲在三氯氧磷中反应得到2-氨基-5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑(1), 然后分别采用超声辐射法和常规加热法与(未)取代苯甲酰基异硫氰酸酯(2)反应合成了一系列未见报到的1-[(未)取代苯酰基-3-[5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑-2-基]-硫脲(3a~3j). 化合物的结构经元素分析, IR, 1H NMR确证. 相似文献
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LI Feng-Yun ZHU Yu-Jie FAN Zhi-Jin XU Jing-Hua GUO Xiao-Feng ZONG Guang-Ning SONG Hai-Bin 《结构化学》2015,34(5)
The title compound 2-(1-(3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carbonyl)piperidin-4-yl)-N-isopropylthiazole-4-carboxamide(C21H22Br Cl N6O2 S,Mr = 536.04) has been synthesized,and its structure was characterized by IR spectra,1H-NMR,13C-NMR,EA,and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic system,space group P/c with a = 15.146(3),b = 11.573(2),c = 26.937(5) ?,β = 103.64(3)°,V = 1839.0(6) ?3,Z = 4,Dc = 1.557 g/cm3,μ(Mo Ka) = 0.71073 mm-1,F(000) = 2192,R = 0.0601 and w R = 0.1392.There exist one intramolecular hydrogen bond at N–H···N and four intermolecular weak interactions at O(2)···H(1),Cl(1)···H(12),O(1)···Cl(1) and S(1)···O(2).Bioassay results indicated that the title compound had good fungicidal and antiviral activities against tobacco mosaic virus. 相似文献
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S. Satyanarayana Reddy 《合成通讯》2013,43(9):1305-1311
Ethyl [2-(2H-chromene-3yl)-4-oxo-1,3-thiazolidin-3yl]acetates (6a–e) were synthesized in a single pot by the reaction of 2H-3-chromenecarbaldehydes (3a–e), glycine ethyl ester hydrochloride (4), and mercaptoacetic acid (5) in diisopropylethylamine/benzene under refluxing conditions in a Dean–Stark trap. 相似文献
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Reactions of 3-methyl-6-[4-(4-hydroxyphenyl)-1-piperazinyl]-2(3H)-benzoxazolone, 3-methyl-6-[4-(4-hydroxy-phenyl)-1-piperazinyl]-2(3H)-benzothiazolone and 1,3-dimethyl-5-[4-(4-hydroxyphenyl)-1-piperazinyl]-2(3H)-benzimidazolone with cis-{[2-(2,4-dichlorophenyl) -2-(1H-imidazol-1-ylmethyl)]-1,3-dioxolan-4-yl}methyl meth-anesulfonate in the presence of sodium hydride furnish the title compounds. 相似文献
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The title compound(zifaxaban 2, C20H16ClN3O4 S, Mr = 429.87) was synthesized and its crystal structure was determined by single-crystal X-ray diffraction. Zifaxaban crystallizes in monoclinic, space group P21 with a = 5.7900(12), b = 13.086(3), c = 12.889(3) A, β = 100.86(3)°, V = 959.1(3) A3, Z = 2, Dc = 1.489 g/cm3, F(000) = 444, μ = 0.342 mm-1, the final R = 0.0320 and wR = 0.0640 for 2717 observed reflections(I 2σ(I)). The absolute configuration of the stereogenic center in the title compound was confirmed to be S by single-crystal X-ray diffraction. Four existing intermolecular hydrogen bonds help to stabilize the lattice and the molecule in the lattice to adopt an L-shape conformation. Zifaxaban was slightly more active than rivaroxaban 1 in in vitro assay against human FXa and therefore is promising as a drug candidate. 相似文献