共查询到20条相似文献,搜索用时 78 毫秒
1.
2.
4.
5.
6.
1,2,3—噻二唑衍生物的合成及其生物活性 总被引:2,自引:0,他引:2
自1976年Arndt等合成植物生长调节剂噻苯隆[1]似来,有关含1,2,3一噻二唑化0合物的生物活性的研究就不断有报道[2~5].为了寻找新的具有较好生物活性的化合物,本文以5-氨基-1,2,3-噻二唑为中间体合成了5种不同取代基的磺酰脲类化合物、3种SChiff碱类化合物及吡唑类、酰亚胺类化合物各1种,共10种新化合物.其反应式如下:1实验部分MT-3型元素分析仪;Schimadzu-IR-435型红外光谱仪,KBr压片;Jeolfx-90Q型或BrukerAC-P200型核磁共振仪(CDCI。,DMSO-de,TMS);VGZAB-HS型质谱仪;Yanaco熔点仪(温度计未经校正)… 相似文献
7.
以3-甲基-2-硝基苯甲酸甲酯为起始原料,经两步反应制得中间体1H-吲唑-7-甲酸甲酯(3); 3分别与三氯氧磷、液溴和碘单质反应制得3的3-位卤代产物(4b~4d); 4d与氟试剂或氰化锌反应制得3-氟(氰基)-3(4a和4e); 4d与苯硼酸或甲基硼酸在四三苯基磷钯催化下反应制得3-甲基(苯基)-3(5a和5b);以氢化钠为碱,3, 4a~4c, 4e, 5分别与4-甲烷磺酰氧基哌啶或3-甲烷磺酰氧基四氢吡咯经缩合反应制得3的2,3-位取代产物(6a~6n); 6a~6n在甲醇中氨解,随后采用氯化氢气体脱去Boc保护基合成了14个新型吲唑类PARP-1抑制剂(7a~7n),其结构经1H NMR和ESI-MS表征。生物活性评价结果显示,有7个目标化合物对PARP-1酶活性抑制IC50低于30 nmol·L-1,其中2-(四氢吡咯-4-基)-2H-吲唑-7-甲酰胺(7e)和3-氟-2-(四氢吡咯-4-基)-2H-吲唑-7-甲酰胺(7f)的IC50分别为4.2 nmol·L-1和4.6 nmol·L-1。 相似文献
8.
9.
10.
以2,6-二氟苯腈与吗啉反应制得2-氟-6-吗啉-苯腈(1); 1与水合肼在N-甲基吡咯烷酮中通过环合反应制得3-氨基-4-吗啉-1H-吲唑(2); 2与不同羧酸经缩合反应合成了8个新型吲唑类化合物(4a~4h),其结构经1H NMR, IR和HR-ESI-MS表征。抗肿瘤活性测试结果表明:3,4,5-三甲氧基-氮-(4-吗啉-1H-吲唑-3-基)苯甲酰胺(4a)的抗肿瘤活性最好,对K-562, SMMC7721和T-47D肿瘤细胞有明显抑制作用,IC50分别为0.056 μmol·L-1, 0.062 μmol·L-1和0.078 μmol·L-1。 相似文献
11.
槲皮素衍生物的合成及生物活性研究进展 总被引:2,自引:0,他引:2
综述了槲皮素衍生物的合成及生物活性研究进展,介绍了国内外槲皮素氨基酸类、糖苷类、酯类、醚类衍生物及金属配合物的合成方法及其生物活性研究现状.指出槲皮素是一种从天然植物中提取的黄酮醇类化合物,具有抗氧化,抗菌,扩张血管,抗肿瘤及抗突变等多种生物学活性.然而,槲皮素具有水溶性差、生物利用度较低等缺点,临床应用受到限制.为此,国内外学者对其结构进行修饰改造,开发出了一系列具有新颖结构的槲皮素先导化合物,可望为新型槲皮素衍生物的设计合成提供参考. 相似文献
12.
13.
14.
Feng-Yun Li Xiao-Feng Guo Zhi-Jin Fan Yu-Qing Zhang Guang-Ning Zong Xiao-Lin Qian Liu-Yong Ma Lai Chen Yu-Jie Zhu Kalinina Tatiana Yury Yu. Morzherin Nataliya P. Belskaya 《中国化学快报》2015,26(10):1315-1318
A series of novel 2-amino-1, 3-thiazole-4-carboxylic acid derivatives were designed and synthesized. Their structures were confirmed by melting points, IR, 1H NMR, 13C NMR, and HRMS or elemental analysis. Biological activities of all title compounds including fungicidal activity and antivirus activity were evaluated systematically. Preliminary bioassays indicated that these compounds exhibited good fungicidal activity at 50 μg/mL, compounds 4b and 4i exhibited over 50% activity against six fungi tested. Most compounds showed good activity against TMV with different models in vivo at 100 μg/mL. Compounds 4c and 4e stood out with high effects against TMV in vivo in all models tested, including protective, inactivative, curative, and inductive activities. These data demonstrate a new strategy for fungi and virus control. 相似文献
15.
This review deals with the synthesis, reactions and biological activity of pyrazoloquinazoline derivatives. Some of these reactions have been used successfully to the production of biologically importance compounds. The main purpose of this review is to present a survey of the literature on the chemistry of pyrazoloquinazolines and provides useful applications for these compounds. 相似文献
16.
A series of novel amide derivatives bearing an indazole moiety were synthesized and evaluated for their in vitro S-adenosyl-L-homocysteine hydrolase (SAHase) inhibitory activity. Among these compounds, 8b, 8m, 8r and 8w showed better or similar inhibitory effects compared to the positive control aristeromycin. These results provide a novel lead for the discovery of more potent non-adenosine analogs as SAHase inhibitors. 相似文献
17.
Li-Yuan Zhang Bao-Lei Wang Yi-Zhou Zhan Yan Zhang Xiao Zhang Zheng-Ming Li 《中国化学快报》2016,27(1):163-167
A series of fluorine-and piperazine-containing 1,2,4-triazole thione derivatives were synthesized by the Mannich reaction of triazole intermediates with various substituted piperazines and formaldehyde in high yields. Structures of title compounds were confirmed by melting points, IR, 1H NMR, 13C NMR and elemental analysis. The preliminary bioassays for 17 novel title compounds showed that several compounds have significant fungicidal activity against Cercospora arachidicola, Physalospora piricola and Rhizoctonia cerealis at 50μg/mL. 相似文献
18.
Baolei Wang Yi Ma Yonghong Li Suhua Wang Zhengming Li 《Frontiers of Chemistry in China》2009,4(2):186-190
Ketol-acid reductoisomerase(KARI) is a promising target for the design of herbicides yet there are only few reports on the
molecular design of KARI inhibitors. In this paper, based on the reported 0.165 nm high resolution crystal structure of the
spinach KARI complex, 279 molecules with low binding energy toward KARI were obtained from an MDL/ACD 3D database search using
the program DOCK 4.0. According to the structural information of 279 molecules provided, some amide compounds have been designed
and synthesized. The bioassay results show that most of these amides had inhibitory activity to rice KARI at a test concentration
of 200 μg/mL. Among which eight amides, compounds 1 and 6 show 57.4% and 48.1% inhibitory activity to KARI. The herbicidal
activities of these amides were further investigated on di-cotyledonous rape (Brassica campestris) and mono-cotyledonous barnyardgrass (Echinochloa crusgalli). Compounds 1 and 6 were more favorable than others and showed 52.0% and 72.6% inhibitory activity on rape root at 100 μg/mL
concentration, respectively. These amides could be further optimized for finding more potent candidates.
__________
Translated from Chemical Journal of Chinese Universitiers, 2008, 29(3) (in Chinese) 相似文献
19.
20.
In order to search for novel fungicides with high activity, a series of heteroaryl pyrazoles were synthesized from 5-pyra-zole formhydrazide. The structures of all new compounds were confirmed by spectroscopic methods and microanalyses. Preliminary bioassays indicated that some compounds showed fungicidal activity against Puccinia tritinia and PGR activity as well. 相似文献