SYNTHESIS-STUTTGART
·
2019
·Vol. 51
·期 16
·3085-3090
·
IF 2.867
Menglan Wang,Yudong Li,Qing-An Wu,Shuping Luo,Yuehui Li
Indole scaffold synthesis relies primarily on oxidative C–H amination of N-protected alkenylanilines for C–N intramolecular cyclization reactions. Herein, for the first time, without N-protection, various readily prepared 2-alkenylanilines were transformed into the desired indole products in good yields by using K2S2O8 as oxidant in the presence of catalytic amounts of FeF2. The K2S2O8/FeF2 system offers a direct and benign synthetic route to 3-arylindoles and it is applicable to a wide range of substituted indoles including drug intermediates.
✓ 已验证
产品关联
DOI
高影响因子
SYNTHESIS-STUTTGART
·
2019
·Vol. 51
·期 23
·4425-4433
·
IF 2.867
Yong Jian,Ming Chen,Chao Yang,Wujiong Xia
A small molecule, namely nitroacenaphthene, is reported for the first time as a recyclable visible-light photocatalyst for the construction of the C=N bond from sulfonyl azides and amines. This scalable, site-selective protocol provides a convenient way to access various sulfonyl amidines under mild conditions. Two reaction pathways are proposed, according to different transformation patterns.
✓ 已验证
DOI
高影响因子
PLANTA MEDICA
·
2017
·Vol. 84
·期 05
·336-343
·
IF 2.342
Yifan Wang,Liangjin Xu,Wen Gao,Lixin Niu,Chunyue Huang,Peiming Yang,Xiao Hu
Three new Diels-Alder adducts, macrourins E – G (1–3), one new 2-arylbenzofuran, macrourin H (4), and eight known Diels-Alder adducts (5–12) were isolated from Morus macroura. Their structures were elucidated through extensive analysis of spectroscopic data. The 1H NMR and ECD trends in the determination of the configurations of these Diels-Alder adducts were summarized. The tyrosinase inhibitory activities of all compounds isolated were evaluated, and the new compounds (1–4) as well as the eight known compounds (5–12) were found to be potent with IC50 values ranging from 0.39 to 4.54 µM. Among them, 1 showed the best tyrosinase inhibitory activity with an IC50 value of 0.39 µM, approximately 50 times stronger than the positive control, kojic acid.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Drug Research
·
2017
·Vol. 68
·期 05
·270-279
·
IF 0
Shuoye Yang
Long-circulating liposomal delivery systems of encapsulated Coenzyme Q10 (CoQ10), a ubiquinone anti-cataract agent, were developed with different molar ratios of PEGylated lipids and/or cholesterol. The resulting samples were contrasted through observation of morphology, analysis of particle size and Zeta potential, and in vivo pharmacokinetics. A protamine aggregation method with high selectivity was developed to determine the encapsulation efficiency (EE), after which the liposome formulation was further optimized by applying a Box Behnken design (BBD) using EE as the evaluation index. The results showed that liposomes had a large, unilamellar structure, and that particle sizes of cholesterol-containing liposomes increased along with the increase of cholesterol molar percentage, while the size of PEGylated vesicles decreased slightly as PEG-lipid contents increasing. The optimum formulation and optimal values of each influencing factor were quantitatively obtained, and the measured value was highly consistent with the predicted results. In vivo evaluation performed by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) demonstrated that liposomal encapsulation largely prolonged half-lives and improved bioavailability for vectors prepared with either lipid component, and the liposomes composed of both cholesterol and PEG-lipid possessed the best pharmacokinetic properties. The results suggest that incorporating high contents of cholesterol and PEG modification could be a potentially useful method for enhancing the length of circulation and the sustained release effect for liposome-encapsulated chemicals.
✓ 已验证
产品关联
DOI
PubMed
SYNTHESIS-STUTTGART
·
2022
·Vol. 54
·期 09
·2258-2266
·
IF 2.969
Bao Gao,Xiaojun Liu,Qian Yan,Ruiting Yang,Tao Jiang,Xiuli Zhang
A novel and convenient method for the highly chemoselective synthesis of β-hydroxysulfides mediated by DMSO is reported. This eco-friendly reaction was amenable to a broad range of substrates and provided the desired β-hydroxysulfides in moderate to good yields with high selectivity via radical process. Moreover, several pharmaceutical and bioactive molecules were also suitable substrates for this reaction conditions to afford the targeted products in good yields.
✓ 已验证
DOI
高影响因子
SYNLETT
·
2011
·Vol. 2012
·期 01
·145-149
·
IF 2.447
Wenpeng Mai,Jinwei Yuan,Zhicheng Li,Gangchun Sun,Lingbo Qu
All articles of this category A novel direct arylation of pyridine N -oxideswith arylboronic acids through C-H functionalization hasbeen developed. This new reaction is performed at room temperatureusing catalytic silver(I) nitrate in the presence of potassium persulfateand give 2-pyridyl arylation derivatives of pyridine N -oxides.
✓ 已验证
产品关联
DOI
高影响因子
PLANTA MEDICA
·
2016
·Vol. 83
·期 07
·624-630
·
IF 1.99
Yi-Lin Zhang,Jia-Wen Xu,Xiong-Hao Wu,Peng-Xiao Chen,Fang Wei,Dong-Dong Gao,Xiao-Wen Chen,Yu-Li Luo,Yun-Xin Zhu,Jiehong Huang,Ya-Xia Tan,Lei Zhao,Wen-Liang Zhou
Sodium tanshinone IIA sulphonate, a water-soluble derivative of tanshinone IIA, has been proven to possess versatile biological properties, but its pharmacological effect on tracheal smooth muscle remains elusive. This paper presents a study on the relaxant effect and underlying mechanisms of sodium tanshinone IIA sulphonate on mouse tracheal smooth muscle. The relaxant effect of sodium tanshinone IIA sulphonate was evaluated in mouse tracheal rings using a mechanical recording system. Intracellular Ca2+ concentration was measured in primary cultured tracheal smooth muscle cells using confocal imaging system. The results showed that sodium tanshinone IIA sulphonate induced dose-dependent relaxation of mouse tracheal rings in a β-adrenoceptor- and epithelium-independent manner. Pretreatment with the ATP-sensitive K+ channel blocker glibenclamide partly attenuated the relaxation response. Administration of sodium tanshinone IIA sulphonate notably inhibited the extracellular Ca2+-induced contraction. High KCl or carbachol-evoked elevation in the intracellular Ca2+ concentration was also abrogated by sodium tanshinone IIA sulphonate in tracheal smooth muscle cells. In conclusion, the tracheal relaxant effect of sodium tanshinone IIA sulphonate was independent of β-adrenoceptor and airway epithelium, mediated primarily by inhibition of extracellular Ca2+ influx via L-type voltage-dependent Ca2+ channels and partially by activation of the ATP-sensitive K+ channel. These results indicate the potential therapeutic value of sodium tanshinone IIA sulphonate for asthma treatment.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PLANTA MEDICA
·
2016
·
IF 1.99
Min Li,Fen Liu,Yong-Ri Jin,Xiao-Zhong Wang,Qian Wu,Ying Liu,Xu-Wen Li
Five new triterpenoid saponins (1–5) and four known triterpenoid saponins, ginsenoside Re5 (6), majonoside R1 (7), 24(R)-majonoside R1 (8), and ginsenoside Rf (9), were isolated from the rhizomes of Panacis majoris. The structures of new compounds were elucidated as (20S,24S,25R*)-6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-20,24-epoxy-3β,6α,12β,25,26-pentaol (1), (20S,24R,25R)-6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-20,24-epoxy-3β,6α,12β,25,26-pentaol (2), (20S)-6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-20,25-epoxy-3β,6α,12β,24α-tetraol (3), 6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-3β,6α,12β,20S,24R,25-hexaol (4), and 6-O-[β-D-glucop-yranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-25(26)-ene-3β,6α,12β,20S,24R-pentaol (5) on the basis of extensive spectral analysis and chemical methods. Ginsenoside Re5 was isolated from the plant for the first time. The similarities of the nine compounds lie in the fact that their aglycones are conjoined with the same glucopyranose moieties, the same linkage of the glycosyl chains, and the same glycosylation sites, while they have a varied C-17 side chain. Compounds 3 and 5 exhibited moderate antiplatelet aggregation activities induced by adenosine diphosphate with IC50 values of 23.24 and 18.43 µM, respectively. Compound 5 displayed moderate inhibition of arachidonic acid-induced platelet aggregation with an IC50 value of 30.11 µM.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PLANTA MEDICA
·
2016
·Vol. 82
·期 03
·230-237
·
IF 1.99
Xueli Zhang,Jiajia Lv,Liling Wang,Hua Shao
Taxanes are a class of bioactive compounds isolated from the Taxus species. 10-Deacetylbaccatin III is one of the popular taxane compounds with antitumor activity, but the pharmacokinetic profile of this compound remains elusive. Previously, we prepared the taxane fractions from the twigs and leaves of Taxus chinensis var. mairei containing 20.4 % 10-deacetylbaccatin III. This study aimed to investigate the pharmacokinetics of 10-deacetylbaccatin III and biodistribution, and explore the potential changes when it was administered in the form of taxane extracts. A simple, sensitive, and reliable liquid chromatography-tandem mass spectrometry method was developed and validated for the quantitative determination of 10-deacetylbaccatin III in biosamples. The results showed that 10-deacetylbaccatin III, after oral dosing, displayed a quick absorption into the blood and distribution into major organs. Oral administration of 10-deacetylbaccatin III in the form of taxane mixtures led to a 16-fold increase in the systemic exposure of pure 10-deacetylbaccatin III, with the AUC0-U in the plasma increasing from 25.75 ± 11.34 to 231.36 ± 70.12 µg h/L (p T. chinensis var. mairei, which contributed to an enhanced systemic exposure of pharmacologically active taxanes.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SYNTHESIS-STUTTGART
·
2017
·Vol. 49
·期 08
·1867-1873
·
IF 2.65
Jun Gu,Canbin Qiu,Wenbin Lu,Qun Qian,Kunhua Lin,Hegui Gong
The use of pyridine as the sole ligand for the reductive vinylation of unactivated secondary alkyl halides under Ni-catalyzed conditions has been developed. Both alkyl- and aryl-substituted vinyl bromides are suitable, in which alkyl-decorated α-alkenyl bromides resulted in the α-products in good results.
✓ 已验证
产品关联
DOI
高影响因子
PLANTA MEDICA
·
2017
·Vol. 84
·期 02
·123-128
·
IF 2.342
Fang Wang,Huanhuan Zhong,Shiqi Fang,Yunfeng Zheng,Cunyu Li,Guoping Peng,Xinchun Shen
Eupatorium lindleyanum has traditionally been used as folk medicine in Asian countries for its therapeutic effects on tracheitis and tonsillitis. Investigation of the anti-inflammatory active constituents from E. lindleyanum led to the isolation of two novel sesquiterpene lactones, named eupalinolide L (1) and eupalinolide M (2), and seven known sesquiterpene lactones (3–9). The structures and configurations of the new compounds were determined on the basis of spectroscopic analysis, especially 2D NMR techniques. In vivo experiments showed that the sesquiterpenes fraction significantly reduced mouse ear edema induced by xylene (18.6%, p in vitro assays, compounds 1–9 showed excellent anti-inflammatory activities, as they lowered TNF-α and IL-6 levels in lipopolysaccharide-stimulated murine macrophage RAW 264.7 cells (p E. lindleyanum can be developed as novel potential natural anti-inflammatory agents.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SYNTHESIS-STUTTGART
·
2015
·Vol. 47
·期 19
·3049-3060
·
IF 2.689
Jialin Wang,Jiaqi Liu,Hao Lan,Wenyi Chu,Zhizhong Sun
Intramolecular Friedel–Crafts acylation reactions of 2-arylphenoxyacetic acids are accomplished using trifluoroacetic anhydride or trifluoromethanesulfonic acid at 0 °C or room temperature. Depending on the reaction conditions, dibenzoxepines or arylcoumaranones are obtained in good yields and with high selectivities (83–100%). Plausible mechanistic pathways for the selective formation of the different reaction products are discussed.
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）