共查询到19条相似文献,搜索用时 133 毫秒
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以丙二酸和二氯亚砜为起始原料,经氯代、环合、催化氢化及烷基化反应合成了新化合物——N-甲基-5-苯基-4-羟基-2-吡啶酮,总收率38.7%,其结构经1H NMR,IR和EI-MS表征. 相似文献
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利用手性双唑啉与三氟甲磺酸亚铜催化2-甲氧基苯乙烯与重氮乙酸二环己基甲酯的不对称环丙烷化反应合成了手性环丙烷羧酸酯,用氢氧化钠对其进行选择性水解得到全反式环丙烷羧酸,其ee值经GC测定为88%.进一步经过Curtius重排、烷基化等反应及重结晶等步骤合成了光学纯的具有生理活性的环丙胺化合物1a和1b. 相似文献
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Estevo Silveira Grams Alessandro Silva Ramos Mauro Neves Muniz Raoní S. Rambo Marcia Alberton Perell Nathalia Sperotto Laura Calle Gonzlez Lovaine Silva Duarte Luiza Galina Adilio Silva Dadda Guilherme Arrach Gonalves Cristiano Valim Bizarro Luiz Augusto Basso Pablo Machado 《Molecules (Basel, Switzerland)》2022,27(8)
Tuberculosis remains a global health problem that affects millions of people around the world. Despite recent efforts in drug development, new alternatives are required. Herein, a series of 27 N-(4-(benzyloxy)benzyl)-4-aminoquinolines were synthesized and evaluated for their ability to inhibit the M. tuberculosis H37Rv strain. Two of these compounds exhibited minimal inhibitory concentrations (MICs) similar to the first-line drug isoniazid. In addition, these hit compounds were selective for the bacillus with no significant change in viability of Vero and HepG2 cells. Finally, chemical stability, permeability and metabolic stability were also evaluated. The obtained data show that the molecular hits can be optimized aiming at the development of drug candidates for tuberculosis treatment. 相似文献
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N-(5-邻氯苯基-2-呋喃甲酰氨基)丙氨酰胺衍生物的合成和 生物活性测定 总被引:2,自引:0,他引:2
以5-邻氯苯基-2-呋喃甲酰氯和丙氨酸为起始原料, 通过非均相法得到N-(5-邻氯苯基-2-呋喃甲酰氨基)丙氨酸, 再与10种不同取代苯胺反应, 通过N,N’-二环己基碳二亚胺和4-二甲氨基吡啶(DCC/DMAP)偶合法设计合成了10个未见文献报道的N-(5-邻氯苯基-2-呋喃甲酰氨基)丙氨酰胺类衍生物4a~4j. 通过元素分析, 1H NMR, IR 和MS确定化合物的结构, 初步生物活性测试表明标题化合物具有一定的除草活性. 相似文献
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以2,4-二氯苯甲酸为原料,经酯化、胺化、取代和环合4步反应合成了中间体3-巯基-4-氨基-5-(2,4-二氯)苯基-1,2,4-三唑(4)。以乙腈为溶剂,K2CO3为催化剂,4与2-(2-氯乙酰氨基)-3-甲基-N-丙基苯甲酰胺于室温反应3 h合成了2-[4-氨基-5-(2,4-二氯苯基)-4H-1,2,4-三唑-3-硫亚甲基酰胺]-3-甲基苯甲酰正丙胺,收率78%,其结构经1H NMR,IR,ESI-MS和元素分析确证。 相似文献
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《结构化学》2017,(8)
The title compound N-[5-(benzylthio)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide(C_(16)H_(12)ClN_3OS_2, M_r = 361.86) was designed and synthesized as anticancer agent, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to triclinic, space group P1 with a = 5.7417(10), b = 9.8057(17), c = 14.330(3) ?, a = 91.987(3), b = 97.154(3), γ = 93.402(3)°, V = 798.4(2) ?~3, Z = 2, D_c = 1.505 g/cm~3, μ = 0.507 mm~(-1), F(000) = 372, the final R = 0.0481 and wR = 0.1290 for 2064 observed reflections with I 2s(I). In the crystal packing, the molecules form stacks by a three-dimensional framework, which results from intermolecular N(1)-H(1)···N(2) and C(5)-H(5)···N(3) hydrogen bonds together with π-π stacking interactions between the thiadiazole and chlorobenzene rings. The title compound was found to exhibit more potent in vitro antitumor activities against the four tested cancer cell lines than sorafenib. 相似文献
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以2-(2-硝基苯基)乙腈及4,6-二甲氧基-2-甲磺酰基嘧啶为起始原料,分别经缩合、还原及酰胺化反应合成了6个未见文献报道的N-(2-(腈基(4,6-二甲氧基嘧啶-2-基)甲基)苯基)酰胺类衍生物,其结构经1H NMR、MS和元素分析进行了确证。 在150 g/hm2的用量条件下,合成化合物未显示出除草活性。 在200 mg/L浓度下,部分化合物对黄瓜灰霉病及水稻纹枯病表现出一定的抑菌作用,其中化合物4d对水稻纹枯病的抑制率为72.33%。 相似文献
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