新型15-N-取代苦参碱亚胺衍生物的合成及其抗肿瘤活性

以苦参碱为起始原料，二氯甲烷为溶剂，经三氯氧磷催化与9种芳胺反应合成了一系列新型15-N-取代苦参碱亚胺衍生物(3a~3i)，其结构经¹H NMR， ¹³C NMR 和MS(ESI)表征。采用X-射线单晶衍射仪测定了化合物3a的绝对构型。体外活性测试结果表明：3d和3f对人肝癌细胞HepG2和人宫颈癌细胞HeLa的半数抑制率显著优于苦参碱。     

新型含噻唑和三唑环的亚胺类化合物的合成及生物活性研究

设计合成了一系列新型含有噻唑和三唑环的亚胺类化合物, 其结构经元素分析、1H NMR和X射线晶体衍射确证. 生物活性测试结果表明, 部分化合物在50 μg/L浓度下对苹果轮纹菌具有一定的杀菌活性.     

Microwave‐Assisted Synthesis of Some Novel Benzimidazole Derivatives Containing Imine Function and Evaluation of Their Antimicrobial Activity

4‐Bromo‐o‐phenylenediamine and ethylimido‐p‐bromophenylacetate, 1 , were subjected to microwave irradiation to synthesize benzimidazole derivative, compound 2 . Ester derivative, 3 , and hydrazide derivative, 4 , of compound 2 were also synthesized, respectively. Finally, compound 4 was treated with 11 different aromatic aldehydes to obtain benzimidazole derivatives containing imine function. All reactions were carried out with microwave irradiation and conventional heating, and results were compared. Some of the newly synthesized compounds showed moderate antimicrobial activity against some tested organisms.     

Synthesis of Benzimidazoles via Iron-Catalyzed Aerobic Oxidation Reaction of Imine Derivatives with o-Phenylenediamine

A simple and efficient protocol for preparing benzimidazoles via Fe(NO₃)₃ · 9H₂O-catalyzed aerobic oxidation reaction of imine derivatives with o-phenylenediamine. This process uses air as an economical and green oxidant, tolerates a wide range of substrates, and affords the targeted benzimidazoles in moderate to excellent yields.     

新型含2-取代-1,3-噻唑烷和噻唑环的亚胺类化合物的合成及生物活性

通过4-[(2-氰基亚胺基-1,3-噻唑烷-3-基)甲基]-2-氨基噻唑与取代苯甲醛的缩合反应, 合成了14个新型含2-取代- 1,3-噻唑烷和噻唑环的亚胺类化合物5. 所有化合物的结构均经1H NMR和元素分析确证, 并通过X射线单晶衍射分析测定了化合物5a的晶体结构. 初步生物活性试验结果表明, 部分目标化合物具有一定的杀菌活性和植物生长调节活性.     

Synthesis of 2,6—（substituded）pyridine Derivatives Using Amide and Imine Groups

A new ‘two-armed’ acyclic diamide Ia 2,6-bis(1-ethanecarbozamido-2-amino)pyridine,and a new series of aromatic aldehyde schiff bases containing pyridine ring and arnide bridge,ILa-f, were prepared.The compounds were characterized by elemental analysis,IR,^1HNMR and MS.The bioactivity half inhibitory concentration C1/2 is given.     

喹啉-多胺衍生物的合成及其活性评价

设计合成了13个喹啉-多胺衍生物,产物结构均经1H NMR,ESI-MS和元素分析确认.采用噻唑蓝(MTT)法测试了化合物对连二亚硫酸钠损伤肾上腺嗜铬细胞瘤(PC12)细胞的抑制作用,结果表明所有目标化合物对PC12细胞损伤均有较好的抑制作用,部分化合物优于尼莫地平,其中化合物T6和T7的活性最强,10μmol/L浓度下损伤抑制率分别为28.04%和27.58%.     

新型鸭嘴花碱衍生物的合成及其抗炎活性评价

鸭嘴花碱是从傣药鸭嘴花中分离出来的一种具有多种生物活性的生物碱。对鸭嘴花碱进行结构修饰,经取代和Huisgen反应合成了7个未见文献报道的含三唑取代的鸭嘴花碱衍生物(2a~2g),其结构经1HNMR和13CNMR表征。以地塞米松作阳性对照,采用细菌脂多糖诱导小鼠巨噬细胞RAW264.7模型对衍生物的体外抗炎活性进行了筛...     

丹皮酚噻唑类化合物的合成及其细胞毒性评价

本文以丹皮酚为原料合成了15个新型丹皮酚噻唑衍生物,利用IR、~1H NMR、~(13)C NMR和MS对所得化合物的结构进行表征,采用MTT法考察了目标化合物对MGC-803(胃癌细胞)、LOVO(结肠癌细胞)、T-24(膀胱癌细胞) 3种细胞的体外抗肿瘤活性。结果表明,部分化合物具有良好的细胞毒活性,其中化合物4b、4e、4f、4h、4l对MGC-803的细胞毒性优于阳性对照药顺铂,尤其是化合物4b对MGC-803、LOVO和T-24三种肿瘤细胞的IC_(50)值分别为11. 39±4. 46、2. 06±1. 27和6. 03±0. 86μg/m L,值得进一步研究。     

Synthesis and Antimicrobial Evaluation of Calycanthaceous Alkaloid Derivatives

Chemistry of Natural Compounds - To find pesticidal lead compounds with high activity, a series of new chimonanthine derivatives was synthesized via the introduction of the functional group at the...     

Synthesis and Bioactivity Evaluation of Novel N-Pyridylpyrazolemethanamine Derivatives

To further explore the structure-activity relationship(SAR) of amide bridge moeity of anthranilic diamides derivatives, a series of N-pyridylpyrazole derivatives was designed, synthesized and their biological activities were evaluated. The chemical structures of novel target compounds were confirmed by ¹H nuclear magnetic resonance (NMR), ¹³C NMR and elemental analyses(EA). Bioassay results of insecticidal activity demonstrated that the target compound 6h displayed 70% lethality rate against oriental armyworms at 200 mg/L. Moreover, most compounds displayed moderate to excellent antifungicidal activities against Fusarium oxysporum f. sp. cucumerinum, Cercospora arachidicola Hori, Botryosphaeria dothidea, Alternaria solani, Gibberella zeae and Phytophthora capsici at 50 mg/L. In particular, compound 6e showed 61.5% and 92.3% inhibition rate against Cercospora arachidicola Hori and Botryosphaeria dothidea, which was superior to the commercial positive control Chlorothalonil. These results will provide a potential clue for exploring novel high-effective agrochemicals.     

N-酰基-N''''-茄呢基哌嗪衍生物的合成及生物活性

以茄呢醇为起始原料和茄呢基哌嗪为单元的N-(2-全乙酰葡萄糖基苯甲酰基)-N'-茄呢基哌嗪(5)和N-(2-葡萄糖基苯甲酰基)-N'-茄呢基哌嗪(6),共6个新茄呢基哌嗪衍生物.其结构经元素分析,IR,1H NMR和MS确证.测试了化合物4c,5,6对三种人癌细胞(Bel-7402,KB,HCT-8)的体外生理活性,初步结果表明化合物6比4c和5对三种所测细胞有更好的抑制效果.     

含亚胺基的N-甲氧基氨基甲酸甲酯的合成及其生物活性

以唑菌胺酯为母体,在其侧链上引入亚胺基结构单元,以硫原子替代氧原子,设计并合成了10个新型的N-甲氧基-N-2-[(2-甲基取代苯基亚胺甲基硫亚甲基)苯基]氨基甲酸甲酯,其结构经1H NMR,IR,LC-MS和元素分析表征.初步生物活性测试结果表明,部分化合物对稻瘟病菌和灰霉病菌有较好的抑菌活性.     

Synthesis and Evaluation of Potentiometric Properties of Pyridylthiazole Derivatives

Synthesis of 2-pyridylthiazole ethers 2, 3), 4-nonyl-2-pyridylthiazole 4), 2-nonyl-4-pyridylthiazole 5) and 2-pyridylthiazole imine 6), potentially useful as effective cation-binding ligands, is described. The potentiometric properties of ion-selective membranes prepared with 30–32 wt% PVC, 66 wt% 2-nitrophenyloctyl ether and 2–4 wt% pyridylthiazole derivatives have been examined. While the membranes containing 2-pyridylthiazole ethers 1-4) exhibited high selectivity toward silver(I) ion, that prepared with 2-pyridylthiazole imine 6) resulted in negligible potentiometric reponse to most mono- and divalent cations.     

大黄素衍生物的合成及抗癌活性

通过对大黄素的C6位进行化学修饰, 设计合成了7个含氮杂环的大黄素衍生物和3个含季铵盐基团的大黄素衍生物. 通过红外光谱、 ¹H NMR和质谱表征了所制备化合物的结构, 并测试了它们对白血病细胞Molt-4和淋巴瘤细胞CA46的体外抑制活性. 其中化合物8, 9a+9b, 20a, 20b和20c均显示出比大黄素更高的抗癌活性, 表明苯并咪唑基团和季铵盐基团是大黄素提高抗癌活性的有效药效团.     

Synthesis of New Tetrazole Derivatives and Their Biological Evaluation

Russian Journal of General Chemistry - An operationally simple and efficient method of synthesis of novel 1,5-disubstituted tetrazoles with high yields from easily accessible...     

川芎嗪衍生物的设计、合成及抗血小板凝集活性研究

分别以川芎嗪(TMP)和邻苯二胺为起始原料,经KMn O4氧化、酯缩合、环化、还原等步骤合成了7个新型的川芎嗪衍生物,其结构经1H NMR、13C NMR及HRMS确证。并采用Born比浊法初步测试了化合物的体外抗血小板凝集活性。结果表明,化合物3和7对二磷酸腺苷(ADP)诱导的血小板凝集抑制率IC50分别为0.23mmol/L和0.27mmol/L,优于母体化合物川芎嗪(0.42mmol/L)。     

新型紫杉烷类衍生物的制备及生物活性评价

多药耐药性问题是导致第一代紫杉烷药物在临床化疗失败的主要原因。本文对紫杉醇C7、C10、C14、C3′多个位点的取代基进行改造,针对合成的6个新型的紫杉烷化合物,在体外考察其对多药耐药肿瘤细胞株以及人结肠癌HCT-116干细胞的增殖抑制活性,实验结果表明6个化合物的抗多药耐药活性均优于紫杉醇。采用P-gp高表达的犬肾细胞MDCK-MDR1进一步研究高活性候选化合物JT-3与P-gp的相互作用。以此研发抗多药耐药型的新一代紫杉烷类药物,对开发扩大抗癌新适应症的新一代紫杉烷类抗癌药意义重大。