- Intramolecular Diels-Alder reaction of pyrazines with an alkenyl side chain
-
Intramolecular Diels-Alder reaction of a series of pyrazines bearing a 5-membered-ω-alkene side chain in refluxing trifluoroacetic acid led to the formation of bridged tricyclic compounds. These cycloadducts underwent Retro Diels-Alder reaction in refluxing nitrobenzene to give original pyrazines.
- Chen, Bin,Yang, Chu-Yao,Ye, De-Yong
-
-
Read Online
- Synthesis and antitumor evaluation of one novel tetramethylpyrazine-rhein derivative
-
To discover multi-effective and low toxic anticancer lead compound from traditional Chinese medicine prescription, we synthesized one novel tetramethylpyrazine-rhein derivative which was composed of two main antitumor ingredients of Huazhenghuisheng Pian. The design idea was enlightened by "combination principle" in drug discovery and "compatibility principle" in traditional Chinese medicine. Compound 5's antitumor activity was evaluated by human cancer cell Bel-7402, while the angiogenesis activity was valued by the chick chorioallantoic membrane (CAM) assays. The stability test was carried on artificial gastric juice and artificial intestinal juice; furthermore, compound 5's acute toxicity was evaluated in vivo. The results showed that compound 5 not only displayed antiproliferative activity on Bel-7402 cell (IC50 = 26.4 μM), but also dramatically suppressed normal angiogenesis in chick chorioallantoic membrane. And there was no hydrolysis or structural damage during 24 h in artificial digestive solution. The LD50 value of the compound 5 exceeded 3.2 g/kg by oral administration in mice.
- Wang, Peng-Long,Cheng, Ya-Tao,Xu, Kuo,An, Ya-Wen,Wang, Wei,Li, Qu-Sheng,Han, Qiu-Jun,Li, Qiang,Zhang, Hong-Gui,Lei, Hai-Min
-
-
Read Online
- Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives
-
Rosiglitazone has shown promising anti-inflammation effect. To develop preferable anti-inflammatory agents, twenty-two rosiglitazone analogs were synthesized and their anti-inflammatory activity was evaluated. Among these compounds, 6i and 6k displayed excellent inhibitory activities on the production of inflammatory mediators, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Furthermore, 6i and 6k showed suppression effects on the nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways, and this suppression effects could be partially reversed by GW9662, which is a peroxisome proliferator-activated receptor γ (PPARγ) antagonist. Additionally, our docking results exhibited the well combination of 6i and 6k to PPARγ. So the anti-inflammation activity of 6i and 6k was due at least in part, to their interaction with PPARγ.
- Wang, Fang,Sun, Jun-Rong,Huang, Mei-Yan,Wang, Hui-Ying,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
-
-
Read Online
- Proteomic analysis reveals the potential neuroprotective effects of tetramethylpyrazine dimer in neuro2a/APPswe cells
-
Alzheimer's disease (AD) is a common neurodegenerative disease characterized by pathological processes, including abnormal amyloid deposits and filament tangles, oxidative stress, neuroinflammation, and neurotrophic insufficiency, leading to chronic and prolonged neuronal loss and cognitive deficits. Tetramethylpyrazine (TMP) is one of the main active components of Ligusticum wallichii, a traditional Chinese medicine widely used for brain related disease. Here, we synthesized the TMP derivative tetramethylpyrazine dimer (DTMP), and evaluated the potential mechanisms underlying its potential neuroprotective effects using the murine neuron-like cells (N2a) transfected with the human "Swedish" mutant amyloid precursor protein (N2aAPP). ELISA results indicated that DTMP reduced the levels of Aβ1-40 and Aβ1-42 in N2aAPP. Then through proteomic analysis we identified a total of 208 differentially expressed proteins in N2aAPP cells compared to the wild-type N2a cells (N2aWT), including 144 increased and 64 decreased proteins. 449 differentially expressed proteins were revealed in N2aAPP cells on DTMP treatment with 69 increased and 380 decreased proteins. Bioinformatic analysis suggested that these proteins are enriched in mitochondrial function, the electronic transmission chain, ATP binding, oxidative phosphorylation, GTPase function, the transcriptional translation process, amino acid metabolism, nucleotide binding and others. Given the vital role of mitochondria in the pathogenesis of AD, we selected the electron transport chain pathway-related molecules to further validate these findings. Western-blot analysis demonstrated that DTMP significantly increased the levels of complex I (NDUAA), complex II (SDHB), complex III (UCRI), complex IV (COX5A) and complex V (ATP5A) in N2aAPP cells. The modulation of dysregulated proteins implicated in AD pathogenesis implies the pharmacological mechanisms of DTMP and its potential as a novel therapeutic choice in AD.
- Lin, Xiaoyi,Xu, Benhong,Zhang, Zaijun,Yang, Ying,Liu, Gongping,Zhu, Feiqi,Ren, Xiaohu,Liu, Jianjun,Li, Shupeng,Huang, Xianfeng,Yang, Xifei
-
-
Read Online
- Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C-ring Unit
-
A series of novel oxazolidinone compounds with a substituted ligustrazine C-ring unit and different substituted groups at the C-5 side chain were designed and synthesized using linezolid as a lead and based on a scaffold hopping strategy. Their antibacterial and anti-inflammatory activities were evaluated. The results of in vitro antibacterial assays showed that all fourteen target compounds displayed potent activity against Gram-positive pathogens, particularly 8b, 13b, 14a, 14b, 15a, and 15b. Moreover, 14a and 14b exhibited significant inhibitory activities on the production of inflammatory mediators, including nitric oxide, interleukin-6, and tumor necrosis factor-alpha. Thus, these derivatives could serve as valuable candidates to develop anti-infective agents for the treatment of chronic wounds.
- Chen, Yan,Ruan, Zhi-Xiong,Wang, Fang,Huangfu, De-Sheng,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
-
-
Read Online
- Flavone-ligustrazine compounds CH-X having selective anti-liver cancer effect, preparation method and applications thereof
-
The invention provides a preparation method of a class of flavone-ligustrazine series derivatives, and applications of the flavone-ligustrazine series derivatives in preparation of antitumor drugs. According to the invention, the compound has obvious inhi
- -
-
Paragraph 0035; 0036; 0104; 0105
(2020/03/12)
-
- Application of pyrazine compound in preparation of drugs
-
The invention relates to an application of a pyrazine compound in preparation of drugs. The drugs can be used for treating neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, frontotemporal dementia (FTD), vascular dementia, HIV-related dementia, multiple sclerosis, progressive lateral sclerosis, Friedreich's ataxia, neuropathic pain or glaucoma, inflammation, oxidative damage, and mitochondrial-related diseases.
- -
-
Paragraph 0072-0074
(2020/10/30)
-
- Pyrazine compound and preparation method thereof
-
The invention relates to a pyrazine compound, a stereoisomer, a tautomer and a pharmaceutically acceptable salt thereof, wherein the pyrazine compound, the stereoisomer, the tautomer and the pharmaceutically acceptable salt thereof can treat Alzheimer's disease, Parkinson's disease, Huntington's disease, frontal temporal dementia (FTD), vascular dementia, HIV-related dementia, multiple sclerosis,progressive spinal cord lateral sclerosis, Friedel-Crafts ataxia, neuropathic pain or glaucoma and other neurodegenerative diseases, diabetes mellitus and related diabetic complications, inflammations, oxidative damage and mitochondria-related diseases.
- -
-
Paragraph 0069-0071
(2020/11/09)
-
- Pyrazine derivative, and preparation method and medical use thereof
-
The present invention relates to a pyrazine derivative, and preparation method and medical use thereof. The pyrazine derivative can remove free radicals and suppress calcium overload and has cytoprotective effects, and can be used for the prevention and t
- -
-
Paragraph 0076; 0078
(2019/09/20)
-
- Ginkgolide B Derivative and Preparation Method And Use Thereof
-
Disclosed are a compound as shown in formula I or formula II or a pharmaceutically acceptable salt thereof, wherein R1 is selected from pyrazinyl or substituted pyrazinyl; and R2 is selected from pyrazinyl or substituted pyrazinyl, phenyl or substituted phenyl, alkyl or substituted alkyl.
- -
-
Paragraph 0045
(2019/03/30)
-
- Has anti-tumor effect of the glycyrrhetinic acid derivatives (TOGA - X) of the preparation method and application (by machine translation)
-
The present invention has offered a kind of structure formula 1 compounds and its preparation method and in the preparation of antineoplastic application, the compositions of the invention to liver cancer, stomach cancer, cervical cancer, lung cancer cell
- -
-
Paragraph 0059-0060
(2019/07/11)
-
- Reduction-sensitive nanomicelle and preparation method and application thereof
-
The invention discloses a preparation method and application of a reduction-sensitive nanomicelle, belongs to the technical field of nanomedicine, and particularly provides a preparation method of anamphiphilic prodrug self-assembled nanomicelle of methylpyrazine combined with paclitaxel or docetaxel and application of the nanomicelle in anti-tumor research. Through a nanoprecipitation approach and a dialysis approach, disulfide-bonded ligustrazine and a methylpyrazine analog thereof and the paclitaxel or the docetaxel are adopted for preparing prodrugs which are self-assembled into the nanomicelle, the operation is easy and convenient to implement, the particle size is small and uniform, the drug loading amount is high, and the nanomicelle can respond to a tumor microreduction environment, so that the tumor selectivity of the paclitaxel is improved, the effect of targeted treatment of tumors is achieved, the enrichment of drug concentration at tumor sites is improved, and the nanomicelle achieves good synergism and toxicity reduction effects in in-vivo and in-vitro anti-tumor application.
- -
-
-
- Ligustrazine/azoonium diol salt derivative as well as preparation method and application thereof
-
The invention discloses a ligustrazine/azoonium diol salt derivative as well as a preparation method and application thereof. The derivative has a structure as shown in a formula (I) which is described in the specification, wherein R1 and R2 are the same or different; the R1 and R2 are the same or different and independently represent a hydrogen atom and a C1-C4 alkyl group, and the R1 and R2 forma 5- to 7-membered aliphatic heterocyclic ring or aromatic heterocyclic ring along with the nitrogen atom to which R1 and R2 are connected.; the aliphatic heterocycle or the aromatic heterocycle maybe optionally mono-substituted to penta-substituted by the same or different substituents, the substituents being a C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxyl group, or a halogen. The ligustrazine/azoonium diol salt derivative provided by the invention can inhibit proliferation of tumor cells to different extents. Besides, compared with common breast cancer cells, the ligustrazine/azoonium diol salt derivative provided by the invention has a stronger proliferation inhibition effect on drug-resistant breast cancer cells, and prompts that the ligustrazine/azoonium diol salt derivative has a good application prospect on drug-resistant tumors.
- -
-
-
- Ligustrazine derivative and preparation method and applications thereof
-
The invention provides a ligustrazine derivative and a preparation method and applications thereof. The provided ligustrazine derivative can treat hypoxia damage induced by IAA, can be used to treat stroke and many neurodegenerative diseases, and is capable of promoting the proliferation of neural cells and the growth of cell synapse.
- -
-
Paragraph 0026; 0027
(2018/04/21)
-
- Design, synthesis and biological evaluation of ligustrazine-flavonoid derivatives as potential anti-tumor agents
-
In the clinic some anti-tumor drugs have shown damage to normal blood vessels, which could lead to vascular diseases. Therefore, it is necessary to evaluate the effects of anti-tumor drugs on normal blood vessels at the beginning of the drug design process. In this study, ligustrazine (TMP) and flavonoids were selected as raw materials. Sixteen novel TMP-flavonoid derivatives were designed and synthesized. Interestingly, compounds 14 and 16 were obtained by hydrolysis of a dihydroflavone to a chalcone under alkaline conditions. The cytotoxicity of the TMP-flavonoid derivatives was evaluated on five human tumor cell lines and one classical type of normal endothelial cell lines (HUVEC-12) by an MTT assay. Part of the derivatives showed better anti-tumor activities than the corresponding raw materials. Among them, compound 14 exhibited the closest activity to the positive control against the Bel-7402 cell line (IC50 = 10.74 ± 1.12 μM; DDP IC50 = 6.73 ± 0.37 μM) and had no toxicity on HUVEC-12 (IC50 > 40 μM). Subsequently, fluorescence staining and flow cytometry analysis indicated that compound 14 could induce apoptosis of Bel-7402 cell lines. Moreover, the structure-activity relationships of these derivatives were briefly discussed.
- Wang, Hui,Zhang, Wenxi,Cheng, Yatao,Zhang, Xinyu,Xue, Nannan,Wu, Gaorong,Chen, Meng,Fang, Kang,Guo, Wenbo,Zhou, Fei,Cui, Herong,Ma, Tao,Wang, Penglong,Lei, Haimin
-
-
- Antitumor compound and preparation method thereof
-
Belonging to the technical field of medicine, the invention discloses an antitumor compound and a preparation method thereof, and specifically provides a conjugate of methylpyrazine and paclitaxel ordocetaxel. A disulfide bond is adopted as the connecting bridge for chemical bonding of ligustrazine and its analogue methylpyrazine with paclitaxel or docetaxel. Construction of the amphiphilic compound can improve the water solubility of paclitaxel and docetaxel so as to improve the bioavailability; the active targeting of the disulfide bond can enhance the selectivity of paclitaxel and docetaxel, thereby reducing the lethality to healthy cells and normal tissues; after release of the conjugate when it reaches a target site, ligustrazine can assist paclitaxel and docetaxel in playing an antitumor role together, while the drug resistance is improved, the antitumor effect is enhanced.
- -
-
-
- Ligustrazine-butyphthalide combination compound, preparation method of ligustrazine-butyphthalide combination compound, and application of ligustrazine-butyphthalide combination compound to pharmaceuticals
-
The invention discloses a ligustrazine-butyphthalide combination compound, a preparation method of the ligustrazine-butyphthalide combination compound and an application of the ligustrazine-butyphthalide combination compound to pharmaceuticals. The ligustrazine-butyphthalide combination compound has the following structural formula I as in the description. The phthalic anhydride and the ligustrazine are taken as starting materials, bromization, nucleophilic addition, catalytic dehydration, ester hydrolysis, reduction and esterification reactions are conduced to prepare the ligustrazine-butyphthalide combination compound; a pharmaceutical composition takes the ligustrazine-butyphthalide combination compound as an active pharmaceutical ingredient and is a pharmaceutically acceptable carrier, excipient, diluent, adjuvant, intermedium or a composition. The prepared ligustrazine-butyphthalide combination compound has an excellent effect of inhibiting in-vitro platelet aggregation (ADP) induced platelet aggregation, has a better in-vivo pharmacokinetics properties, and can be used for preventing and treating cardiovascular and cerebrovascular diseases, vascular senile dementia and the complications.
- -
-
Paragraph 0028; 0032
(2017/08/30)
-
- A Radix Salviae Miltiorrhizae su-amide derivatives and its preparation and use
-
The invention discloses a tanshinol amide derivative and a preparation method and application thereof. A structural general formula of the tanshinol amide derivative is shown as a general formula (I) and a general formula (II). The tanshinol amide derivative can be used for preparing medicines for treating the ischemic cerebrovascular disease and the vascular dementia.
- -
-
Paragraph 0058-0061
(2018/01/19)
-
- A deuterium generation of niter alkone qin compound and its preparation method and application in pharmacy (by machine translation)
-
The invention relates to a deuterium generation of niter alkone qin compound and its preparation method and application. The compound has the following general formula (I) of the structure. Such compounds [...] prototype compound compared with better stability, increased activity, with nerve protection, can be used for nerve degenerative diseases such as cerebral apoplexy, Alzheimer's disease (AD), Parkinson's disease (PD), brain injury (TBI) prevention and treatment of such diseases. (by machine translation)
- -
-
Paragraph 0036; 0037
(2017/12/28)
-
- Design, synthesis, and biological evaluation of novel tetramethylpyrazine derivatives as potential neuroprotective agents
-
Oxidative stress plays a crucial role in neurological diseases, resulting in excessive production of reactive oxygen species, mitochondrial dysfunction and cell death. In this work, we designed and synthesized a series of tetramethylpyrazine (TMP) derivatives and investigated their abilities for scavenging free radicals and preventing against oxidative stress-induced neuronal damage in vitro. Among them, compound 22a, consisted of TMP, caffeic acid and a nitrone group, showed potent radical-scavenging activity. Compound 22a had broad neuroprotective effects, including rescuing iodoacetic acid-induced neuronal loss, preventing from tert-butylhydroperoxide (t-BHP)-induced neuronal injury. Compound 22a exerted its neuroprotective effect against t-BHP injury via activation of the phosphatidyl inositol 3-kinase (PI3K)/Akt signaling pathway. Furthermore, in a rat model of permanent middle cerebral artery occlusion, compound 22a significantly improved neurological deficits, and alleviated the infarct area and brain edema. In conclusion, our results suggest that compound 22a could be a potential neuroprotective agent for the treatment of neurological disease, particularly ischemic stroke.
- Chen, Haiyun,Tan, Guolian,Cao, Jie,Zhang, Gaoxiao,Yi, Peng,Yu, Pei,Sun, Yewei,Zhang, Zaijun,Wang, Yuqiang
-
-
- Triterpenoid derivative TBA-X with antitumor effect as well as preparation method and application thereof
-
The invention provides a compound with a structural general form 1 or 2, a preparation method thereof, and an application of the compound in preparation of antitumor drugs. The composition provided by the invention has a significant inhibitory action on liver cancer, stomach cancer, colon cancer, cervical cancer cell lines.
- -
-
Paragraph 0055; 0056; 0088; 0089
(2017/08/28)
-
- He pyrrole testsamine synonym, preparation method and its application
-
The invention relates to the field of medicinal chemistry and particularly relates to picotamide analogues (I), a preparation method and a pharmaceutical composition containing the picotamide analogues, wherein R represents hydrogen, 3, 5, 6- trimethyl, 5-methyl or 6-methyl. The picotamide analogues provided by the invention can be used for treating or preventing thromboembolic diseases.
- -
-
Paragraph 0030; 0032-0034
(2017/03/08)
-
- New uses of tetramethylpyrazine derivative in biological nerve protection
-
The present invention provides applications of a tetramethylpyrazine derivative having a structure represented by a formula 1, or a salt thereof, or a composition containing a tetramethylpyrazine derivative having a structure represented by the formula 1 or a salt thereof in preparation of drugs for prevention or treatment of nervous system diseases, wherein R1 is any one selected from -H, -OCH3 and -OH, R2 is any one selected from -H, -OCH3 and -OH, R3 is any one selected from -H, -OCH3, -OH and -CH3, and R4 is any one selected from -H and -OCH3. The present invention further provides a tetramethylpyrazine derivative having a structure represented by a formula 2, or a salt thereof, or a composition containing a tetramethylpyrazine derivative having a structure represented by the formula 2 or a salt thereof in preparation of drugs for prevention or treatment of nervous system diseases, wherein R1 is any one selected from -H, -OH and -OCOCH3, R2 is any one selected from -H, -OCH3 and -OH, and R3 is any one selected from -H and -OH. The formulas 1 and 2 are defined in the specification.
- -
-
Paragraph 0028; 0037; 0038
(2016/10/10)
-
- Preparation method and application of antitumor drug X-TOA
-
The invention provides a preparation method of compounds with the structure represented by general formula 1, and an application of the compounds in the preparation of antitumor drugs. The compounds are prepared through ester bond condensation of a 3th hy
- -
-
Paragraph 0084; 0085
(2016/10/17)
-
- Synthesis and biological evaluation of T-OA analogues as the cytotoxic agents
-
Abstract The lead compound T-OA, 3β-hydroxyolean-12-en-28-oic acid-(3,5,6-trimethylpyrazine-2-yl) methyl ester, which exhibited promising anticancer effects in vitro and in vivo, has previously been reported. According to the structural features, a series of novel T-OA analogues were synthesized via amino condensation reaction. These analogues' cytotoxic activities were evaluated on five cancer cell lines (Bel-7402, HepG-2, HT-29, Hela, BGC-823) and hepatic stellate cell line (HSC-6). Among the candidates, compounds 8 and 16 showed promising effects; 3β-hydroxy-lup-20(29)-ene-28-oic acid-(3,5,6-trimethylpyrazin-2-yl) methyl amine (16) even possessed superior bioactivities to positive drugs (cisplatin and ursolic acid), which was worthy of further study. In addition, structure-activity relationships and Clog P values of T-OA analogues were briefly discussed.
- Xu, Kuo,Xu, Xin,Chu, Fuhao,Wang, Mina,Wang, Penglong,Li, Guoliang,Song, Jixiang,Zhang, Yuzhong,Lei, Haimin
-
p. 6257 - 6269
(2015/08/18)
-
- Medicine for Treating Ischemic Brain Injury and its Sequelae, and Preparation Method Thereof
-
Disclosed in the present invention are a compound of the general structure formula LQC-T as shown below, wherein R represents an aromatic organic acid or phenol or the structural analogue thereof, such as protocatechuic acid, protocatechuic aldehyde, vani
- -
-
Paragraph 0070
(2014/02/15)
-
- SYNTHESIS AND USE OF ANTI-TUMOR DRUG LQC-Y
-
Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 m
- -
-
Paragraph 0106
(2014/02/15)
-
- Amino acid derivatives of ligustrazine-oleanolic acid as new cytotoxic agents
-
A series of novel ligustrazine-oleanolic acid (TOA) derivatives were designed, and synthesized by conjugating amino acids to the 3-hydroxy group of TOA by ester bonds. Their cytotoxicity was evaluated on four cancer cell lines (HepG2, HT-29, Hela and BGC-823) by standard MTT assays. The ClogP values were calculated by means of computer simulation, and logP values of both 3β-glycine ester olean-12-en-28-oic acid-3,5,6-trimethylpyrazin-2-methyl ester (6a) and TOA were determined using a shake flask-ultraviolet spectrophotometry method. It was found that 6a and the 3β-L-lysine ester-6g not only displayed good cytotoxicity (IC50 50 = 4.884 μM) had lower nephrotoxicity than both 6g (IC50 = 2.310 μM) and cisplatin (CDDP, IC50 = 3.691 μM) on MDCK cells. Combining Giemsa and DAPI staining, it was further verified that 6a could induce HepG2 apoptosis via nuclei fragmentation and had lower nephrotoxicity. In addition, the structure-activity relationships of these derivatives are briefly discussed.
- Chu, Fuhao,Xu, Xin,Li, Guoliang,Gu, Shun,Xu, Kuo,Gong, Yan,Xu, Bing,Wang, Mina,Zhang, Huazheng,Zhang, Yuzhong,Wang, Penglong,Lei, Haimin
-
p. 18215 - 18231
(2015/01/08)
-
- DANSHENSU AND CHUANXIONGQIN DERIVATIVES, PROCESS FOR PREPARATION, AND USE THEREOF
-
The present invention provides Danshensu derivatives containing a moiety of Chuanxiongqin (tetramethylpyrazine), and pharmaceutical compositions containing the Danshensu derivatives or their salts and pharmaceutically acceptable carriers. The invention also provides methods for preparing the Danshensu derivatives or their salts, and uses of the compositions in manufacture of medicaments for prevention and treatment of diseases or disorders including cardiovascular and cerebrovascular diseases and their complications.
- -
-
Page/Page column 4/9
(2012/08/27)
-
- Novel multi-functional nitrones for treatment of ischemic stroke
-
Ischemic stroke resulting from obstruction of blood vessels is an enormous public health problem with urgent need for effective therapy. The co-administration of thrombolytic/antiplatelet agent and neuroprotective agent improves therapeutic efficacy and agent possessing both thrombolytic/ antiplatelet and antiradical activities provides a promising strategy for the treatment of ischemic stroke. We have previously reported a novel compound, namely TBN, possessing both antiplatelet and antiradical activities, showed significant neuroprotective effect in a rat stroke model. We herein report synthesis of a series of new pyrazine derivatives, and evaluation of their biological activities. Their mechanisms of action were also investigated. Among these new derivatives, compound 21, armed with two nitrone moieties, showed the greatest neuroprotective effects in vitro and in vivo. Compound 21 significantly inhibited ADP-induced platelet aggregation. In a cell free antiradical assay, compound 21 was the most effective agent in scavenging the three most damaging radicals, namely .OH, O2.- and ONOO -.
- Sun, Yewei,Zhang, Gaoxiao,Zhang, Zaijun,Yu, Pei,Zhong, Haijing,Du, Jing,Wang, Yuqiang
-
scheme or table
p. 3939 - 3945
(2012/08/13)
-
- Synthesis and biological evaluation of new ligustrazine derivatives as anti-tumor agents
-
To discover new anti-cancer agents with multi-effect and low toxicity, a series of ligustrazine derivatives were synthesized using several effective anti-tumor ingredients of Shiquandabu Wan as starting materials. Our idea was enlightened by the "combination principle" in drug discovery. The ligustrazine derivatives' anti-tumor activities were evaluated on the HCT-8, Bel-7402, BGC-823, A-549 and A2780 human cancer cell lines. In addition the angiogenesis activities were valued by the chick chorioallantoic membrane (CAM) assay. 1,7-bis(4-(3,5,6-Trimethylpyrazin-2-yl)-3-methoxyphenyl)-1,6-heptadiene- 3,5-dione (4) and 3Ha,12Ha-dihydroxy-5ss-dholanic acid-3,5,6- trimethylpyrazin-2-methyl ester (5) not only displayed antiproliferative activities on these cancer cells, but also dramatically suppressed normal angiogenesis in CAM. The LD50 value of the compound 5 exceeded 3.0 g/kg by oral administration in mice.
- Wang, Penglong,She, Gaimei,Yang, Yanan,Li, Qiang,Zhang, Honggui,Liu, Jie,Cao, Yinqiu,Xu, Xin,Lei, Haimin
-
experimental part
p. 4972 - 4985
(2012/09/21)
-
- LIGUSTRAZINE AROMATIC ACID ETHER DERIVATIVE, ITS PREPARATION METHOD, PHARMACEUTICAL COMPOSITION, AND APPLICATION
-
Ligustrazine aromatic acid ether derivative of general formula I, its preparation method, pharmaceutical composition and application, wherein Ar is selected from aryl substituted aryl and substituted styryl, R is selected from hydrogen and alkyl with no more than 6 carbon atoms.
- -
-
Page/Page column 7
(2010/08/09)
-
- Synthesis of novel ligustrazine derivatives as Na+/H+ exchange inhibitors
-
A novel series of 3,5,6-trimethylpyrazine-2-methoxy (or methylamino) substituted benzoyl-guanidine derivatives were designed and synthesized as Na+/H+ exchange (NHE) inhibitors. In this study, compounds with electron-withdrawing substituents on the benzene ring seemed to improve NHE-1 inhibitory activities. Compounds 6d, 6k, and 6l were found to be potent inhibitors of NHE-1 (IC50=3.0±1.6, 3.0±1.4, and 1.6±0.4nmol/l, resp.). Furthermore, they showed a remarkable reduction of infarct size in the rat myocardial infarction model in vivo.
- Ren, Mei,Dong, Jin,Xu, Yungen,Wen, Nan,Gong, Guoqing
-
experimental part
p. 2727 - 2736
(2011/08/06)
-