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1.
Halise Inci Gul Kaan Kucukoglu Cem Yamali Sinan Bilginer Hafize Yuca Iknur Ozturk 《Journal of enzyme inhibition and medicinal chemistry》2016,31(4):568-573
In this study, 4-(2-substituted hydrazinyl)benzenesulfonamides were synthesized by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13CNMR, and HRMS. Ketones used were: Acetophenone (S1), 4-methylacetophenone (S2), 4-chloroacetophenone (S3), 4-fluoroacetophenone (S4), 4-bromoacetophenone (S5), 4-methoxyacetophenone (S6), 4-nitroacetophenone (S7), 2-acetylthiophene (S8), 2-acetylfuran (S9), 1-indanone (S10), 2-indanone (S11). The compounds S9, S10 and S11 were reported for the first time, while S1–S8 was synthesized by different method than literature reported using microwave irradiation method instead of conventional heating in this study. The inhibitory effects of 4-(2-substituted hydrazinyl)benzenesulfonamide derivatives (S1–S11) against hCA I and II were studied. Cytosolic hCA I and II isoenzymes were potently inhibited by new synthesized sulphonamide derivatives with Kis in the range of 1.79?±?0.22–2.73?±?0.08?nM against hCA I and in the range of 1.72?±?0.58–11.64?±?5.21?nM against hCA II, respectively. 相似文献
2.
Hyoung Jae Lee Bunta Watanabe Masaru Nakayasu Michio Onjo Yukihiro Sugimoto 《Bioscience, biotechnology, and biochemistry》2017,81(12):2253-2260
Fifteen steroidal saponins 1–15, which include 4 furostanol glycosides 1–3 and 15, and 11 spirostanol glycosides 4–14, were isolated from the tubers and leaves of lesser yam (Dioscorea esculenta, Togedokoro). Their structures were identified by nuclear magnetic resonance and liquid chromatography mass spectroscopy. Four steroidal saponins 9, 11, 14, and 15 were found to be novel compounds. 相似文献
3.
Chiemi Moriya Takahiro Hosoya Sayuri Agawa Yasumasa Sugiyama Ikuko Kozone Kazuo Shin-ya 《Bioscience, biotechnology, and biochemistry》2013,77(9):1484-1492
Purple yam (Dioscorea alata L.), which is widely distributed in tropical and subtropical regions, is characterized by its color and viscosity. Previous studies have shown that purple yams contain a variety of acylated anthocyanins that exhibit higher levels of antioxidant activity than the corresponding nonacylated compounds. In this study, the pigments found in purple yams from the Philippines (D. alata) were isolated and evaluated in terms of antioxidant activity. Four new acylated anthocyanins, alanins (1–4) were isolated from the MeOH extracts of purple yam, which were subsequently determined to be cyanidin (1, 2, and 4) and peonidin (3) type compounds, along with four known anthocyanins (5–8). The structures of 1–4 were determined by spectroscopic methods, including NMR and MS analyses. The antioxidant activities of anthocyanins 1–8 were investigated using oxygen radical absorbing capacity and ferric reducing antioxidant power assays. 相似文献
4.
【目的】研究分离自三亚亚龙湾红树林根系土壤的真菌Aspergillus sp. WHUF0343的次级代谢产物及其生物活性。【方法】利用硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备高效液相色谱等技术对该菌的发酵产物进行分离纯化;综合利用核磁共振波谱(NMR)和质谱(MS)等现代波谱技术以及与文献数据对照确定化合物的结构;分别采用肉汤微量稀释检测法和MTS法对化合物进行抗菌和肿瘤细胞毒活性测试。【结果】从真菌Aspergillus sp.WHUF0343的发酵产物共分离并鉴定了10个化合物,分别为isoechinulin A (1)、neoechinulin A (2)、neoechinulin E (3)、preechinulin (4)、neoechinulin D (5)、variecolorin J (6)、dehydroechinulin (7)、questinol (8)、emodin (9)和catenarin (10)。活性评价显示化合物2、9和10对幽门螺杆菌(Helicobacter pylori)和金黄色葡萄球菌(Staphylococcus aure... 相似文献
5.
《Nucleosides, nucleotides & nucleic acids》2013,32(8):1555-1569
Two simple regiospecific methodologies based on triazolic ring construction in the course of synthesis were applied for the synthesis of 1,2,3-triazolic nucleoside analogues. The cycloaddition reactions between diazomalonaldehyde and appropriate glycosylamine derivatives were rather effective, producing the desired nucleosides 11, 17 and 24. Diazotization of enamines 21a and 21b led to the corresponding triazolic ribonucleoside derivatives 22a and 22b, in good yields. Deprotection reaction of 22a, 22b and 24 was easily achieved by Lewis acid catalysis, producing the corresponding ribonucleosides 23a, 23b and 25. 相似文献
6.
Tokumi Maruyama Shigetada Kozai Mayuko Uchida 《Nucleosides, nucleotides & nucleic acids》2013,32(4-5):661-671
Abstract 1-Benzyluracils 2a,b were treated with iodobenzene in the presence of cuprous oxide in 2,4,6-trimethylpyridine at 180°C to give the N 1-phenyl derivatives 3a and 3b in 47% and 55%, respectively. Similar reaction of 2a with 2-bromopyridine at 120°C gave the 3-(2-pyridinyl)uracil 4a in 42% yield. However, unusual product 5 as well as 3-(2-pyridinyl) derivative 4b were obtained in the case of 2b. The structure of 5 was identified as 1-(2,6-difluorobenzyl)-3-[(2,4-dimethyl-2-pyridinyl)methyl]uracil from spectroscopic data. Reaction of the hypoxanthines 7a,b with 2-bromopyridine gave the 1-(2-pyridinyl)hypoxanthines 8a,b in low yields. But N-phenylation of 7a,b were unsuccessful. 相似文献
7.
Antonov AS Kalinovsky AI Dmitrenok PS Kalinin VI Stonik VA Mollo E Cimino G 《Carbohydrate research》2011,346(14):2182-2192
Seven new triterpene glycosides, erylosides R1 (1), T1 (3), T2 (4), T3 (5), T4 (6), T5 (7), and T6 (8) along with the known formoside (2) were isolated from the sponge Erylus formosus collected along the Caribbean coast of Mexico. Glycoside 1 was determined as a trisaccharide, glycoside 2 as a tetrasaccharide while glycosides 3–8 were hexasaccharide. Their carbohydrate chains were unprecedented and have never been found in oligosaccharides from other biological sources, except Erylus spp. Three carbohydrate chains in the glycosides 3 and 6, 4 and 7, 5 and 8 correspondingly are new. The glycosides 1–5 have penasterol as aglycone while glycosides 6–8 proved to be glycoconjugates of 24-methylene-14-carboxy-lanost-8(9)-en-3β-ol. 相似文献
8.
为了解苦槛蓝(Myoporum bontioides)的化学成分,采用色谱分离法从叶中分离得到11个化合物,分别鉴定为:5,7,3’-三羟基-4’-甲氧基黄酮(1)、3,5,7,4’-四羟基-3’-甲氧基黄酮(2)、5,7,4’-三羟基-3’,5’-二甲氧基黄酮(3)、木犀草素(4)、山奈酚(5)、鼠李黄素(6)、5,7-二羟基二氢黄酮(7)、7,4’-二羟基二氢黄酮(8)、5,7,3’,4’-四羟基二氢黄酮(9)、5-O-乙酰基-3,7,3’,4’-四羟基二氢黄酮(10)和7-甲氧基香橙素(11)。除化合物4、7、11之外,其他化合物均为首次从苦槛蓝叶中分离得到。菌丝生长速率法测试表明化合物4、7~9和11对荔枝霜疫霉菌具有较好的抑菌活性。 相似文献
9.
苦槛蓝叶中的黄酮类化合物 总被引:2,自引:0,他引:2
为了解苦槛蓝(Myoporum bontioides A.Gray)的化学成分,采用色谱分离技术从苦槛蓝叶片中分离得到11个黄酮类化合物。通过波谱分析,他们的结构分别鉴定为:桔皮素(1)、甜橙素(2)、5,4′-二羟基-6,7,8,3′-四甲氧基黄酮(3)、4′,5,7,8-四甲氧基黄酮(4)、去甲基川陈皮素(5)、5-羟基-6,7,3′,4′-四甲氧基黄酮(6)、3′,4′,5,6,7,8-六甲氧基黄酮(7)、二氢山柰酚(8)、木犀草素(9)、3′,4′,5,7-四羟基-3-甲氧基黄酮(10)和芹黄素(11)。除化合物9之外,其他化合物均为首次从苦槛蓝叶片中分离得到。孢子萌发法测定结果表明,化合物1,2,8和9对香蕉炭疽菌(Colletotrichum musae)具有较好的抑菌活性。这为苦槛蓝叶片中有效成分的利用提供了理论依据。 相似文献
10.
Yoshiko Sato Kenji Ueyama Tokumi Maruyama Douglas D. Richman 《Nucleosides, nucleotides & nucleic acids》2013,32(1-3):109-119
Abstract Treatment of the 2,3-di-O-benzoate 1 with sodium boronhydride mainly afforded the 3-O-benzoate 2 accompanied with isomers 3a,b and fully deprotected product 4. Compound 2 was converted to 5, from which 8 was obtained. The 1-cyclobutanols 8 and 5 were successfully condensed with 6-chloropurine by Mitsunobu reaction to give 9 and 11, respectively. After partial deprotection, the cyclobutyl nucleosides 10 and 15 were subjected to fluorination using DAST to afford the fluoromethyl analogs 12 and 16 from which target compounds 14 and 17 were obtained in good yields, respectively. 相似文献
11.
Hassan Mansouri-Torshizi Fatemeh Khosravi Khatereh Abdi Sareh Zareian-Jahromi 《Journal of biomolecular structure & dynamics》2013,31(17):4419-4432
AbstractIn this study, four Co(III)-, Cu(II)-, Zn(II)- and Pd(II)-based potent antibacterial complexes of formula K3[Co(ox)3]·3H2O (I), [Cu(phen)2Cl]Cl·6.5H2O (II), [Zn(phen)3]Cl2 (III) and [Pd(phen)2](NO3)2 (IV) (where ox is oxalato and phen is 1,10-phenanthroline) were synthesized. They were characterized by elemental analysis, molar conductivity measurements, UV–vis, Fourier transform infrared (FT-IR) and proton nuclear magnetic resonance (1H-NMR) techniques. These metal complexes were ordered in three combination series of I+II, I+II+III and I+II+III+IV. Antibacterial screening for each metal complex and their combinations against Gram-positive and Gram-negative bacteria revealed that all compounds were more potent antibacterial agents against the Gram-negative than those of the Gram-positive bacteria. The four metal complexes showed antibacterial activity in the order I > II > III > IV, and the activity of their combinations followed the order of I+II+III+IV > I+II+III > I+II. The DNA-binding properties of complex (I) and its three combinations were studied using electronic absorption and fluorescence (ethidium bromide displacement assay) spectroscopy. The results obtained indicated that all series interact effectively with calf thymus DNA (CT-DNA). The binding constant (Kb), the number of binding sites (n) and the Stern–Volmer constant (Ksv) were obtained based on the results of fluorescence measurements. The calculated thermodynamic parameters supported that hydrogen bonding and van der Waals forces play a major role in the association of each series of metal complexes with CT-DNA and follow the above-binding affinity order for the series.Communicated by Ramaswamy H. Sarma 相似文献
12.
《Nucleosides, nucleotides & nucleic acids》2013,32(10-11):1891-1902
Reaction of monosaccharides (D-glucose, D-galactose, D-xylose or L-arabinose) with 6-amino-3-aryl-2-methyl-4-(3H) quinazolinones (1a–c) in boiling methanol yielded the corresponding N-glycopyranosides 3a–c, 4a–c, 5a,b and 6a,b. The N-glycopyranosides 3a–c, 4a–c, 5a,b and 6a,b were acetylated with acetic anhydride and pyridine to give the corresponding acetate derivatives 7a–c, 8a–c, 9a,b and 10a,b. The structures of all these glycosides were assessed by elemental analysis, IR, NMR and mass spectra. Some of these products were tested for anticancer and anti-AIDS activity. 相似文献
13.
Lilliam Casillas-Martinez Millie L. Gonzalez Zamara Fuentes-Figueroa Cyd M. Castro Deborah Nieves-Mendez Carmen Hernandez 《Geomicrobiology journal》2013,30(6):269-281
Seasonal variations in precipitation changed the community composition and microbial activity in a hypersaline, tropical microbial mat, in Cabo Rojo, PR. Using a combination of dissection, light, and transmission electron microscopy, terminal restriction fragment length polymorphism (T-RFLP), in situ microelectrode studies, and 35 S isotope incubations, we documented the major differences between wet and dry seasons. During the wet season (precipitation 177 mm), cyanobacterial (green layer) and anoxyphototrophic (pink layer) communities, as well as the black FeS layer were well-developed, and T-RFLP patterns indicated a diverse community. The rate of oxygenic photosynthesis was 49 μ M min ? 1 . Aerobic respiration was 29 μ M min ? 1 , and sulfate reduction was 264 nmol cm ? 3 h ? 1 . During the dry season (precipitation 51 mm), cyanobacteria and anoxyphototrophs were less diverse and abundant, and T-RFLP patterns were less complex. The O 2 production rate was reduced to 9 μ M min ? 1 , as was O 2 consumption (7 μ M min ? 1 ) and sulfate reduction (26 nmol cm ? 3 h ? 1 ). Aragonite, calcite, halite, and quartz were the predominant minerals. Seasonal differences were found in the green and pink layers for both halite and quartz. Gypsum was not observed, likely due to a sample handling artifact. The fluctuations in community composition and metabolic activity, principally reflected in fluctuations in binding and trapping potential of the uppermost mat community, might be responsible for the observed differences in mineralogy. 相似文献
14.
Yanfa Sun Ranran Liu Xiqing Lu Yaodong Hu Guiping Zhao Maiqing Zheng 《Animal biotechnology》2013,24(1):53-65
The associations between polymorphisms of five genes, calpain 1 ( CAPN1 ), follicle stimulating hormone beta (FSHB), follicle stimulating hormone receptor (FSHR), peroxisome proliferator-activated receptor gamma (PPARG), and retinol binding protein 7 (RBP7), and live weight, carcass composition, and meat-quality traits were estimated from two meat-type chickens lines (n = 311). Except for the variants of the FSHR gene, 11 SNPs of the other four genes and two diplotypes of PPARG were associated with one or more traits excluding shear factor (SF). SNP C31566680T of the CAPN1 gene was significantly associated with live weight (LW) carcass traits. The SNP A4580859C of FSHB gene was significantly associated with breast muscle weight (BrW) and LW. One of the PPARG SNPs, C5070948T, was associated with intramuscular fat content in breast (IMF br ). Diplotype P1 of the PPARG gene was significantly associated with LW and all carcass traits. P3 were significantly associated with abdominal fat weight (AbFW). SNPs in RBP7 were only associated with BrW. These results indicate that the four genes were associated with these traits and have promise as genetic markers for future marker-assisted selection. Supplementary materials for this paper are available online. 相似文献
15.
Kosaku Hirota Yasunari Monguchi Hironao Sajiki Chizuko Yatome Akio Hiraoka Yukio Kitade 《Nucleosides, nucleotides & nucleic acids》2013,32(8):1333-1345
Abstract In expectation of discovering their antiviral activity, acyclic adenosine derivatives 7, 11, 12, and 16 were designed as analogs of neplanocin A (NPA) and L-eritadenine which are strong inhibitors of S-adenosyl-L-homocysteine hydrolase. The 1′,5′-seco-analog of 4′-deoxymethyl-NPA (DHCA) 7 was synthesized by dideoxygenation of 9-(2,3-O-isopropylidene-D-ribityl)adenine (2). Acyclic DHCA analogs 11 and 16 were obtained by Wittig reaction of the aldehyde 3 with Ph3P=CHCO2Et and Ph3P=CHCN, respectively. Hydrolysis of the ester 11 afforded a vinylog of L-eritadenine 12. The synthesized acyclic nucleosides 7, 10, and 11 were evaluated for antiviral activity, however, none of them showed any significant antiviral activity. 相似文献
16.
Biserka Kasnar Dean S. Wise Louis S. Kucera John C. Drach Leroy B. Townsend 《Nucleosides, nucleotides & nucleic acids》2013,32(1-3):459-479
Abstract The synthesis of 4-methoxy-, 4-amino-3-chloro-, and 4-amino-1-(2,3-dideoxy-B-D-glycero-pentofuranosyl)pyridazin-6-one nucleosides, 6,19 and 20 is described. The synthesis of 3,4-dichloropyridazin-6-one (10) was accomplished in 44% overall yield using bromomaleic anhydride (17) as the starting material. The condensation of the silylated base of 10 with the halogenose 12 in the presence of trimethylsilyl triflate as a catalyst afforded a mixture of3,4-dichloro-1-(3,5-di-O-p-toluoyl-2-deoxy-B-D-erythro-pentofuranosyl)pyrridazin-6-one (13) in 67% and its α-anomer 14 in 12% yield, respectively. A series of 3′-sulfonate esters were prepared to explore the synthesis of 3-chloro-4-hydroxy-1-(3-azido-2,3-dideoxy-B-D-erythro-pentofuranosyl) pyridazin-6-one (32) via 6,3-anhydronucleoside analogues. Compounds 15, 19 and 20 were evaluated against human immunodeficiency virus, human cytomegalovirus, and herpes simplex virus type 1 but were inactive. 相似文献
17.
Tai Kaneshima Kazuki Toeda Takane Fujimori Makoto Nishizawa 《Bioscience, biotechnology, and biochemistry》2017,81(8):1461-1465
Various antimicrobial constituents of camu-camu fruit were isolated. Acylphloroglucinol (compound 1) and rhodomyrtone (compound 2) were isolated from the peel of camu-camu (Myrciaria dubia) fruit, while two other acylphloroglucinols (compounds 3 and 4) were obtained from camu-camu seeds. The structures of the isolated compounds were characterized by spectrophotometric methods. Compounds 1 and 4 were confirmed to be new acylphloroglucinols with different substituents at the C7 or C9 position of 2, and were named myrciarone A and B, respectively. Compound 3 was determined to be isomyrtucommulone B. This is the first report of the isolation of 3 from a natural resource. The antimicrobial activities of compounds 1, 3, and 4 were similar to those of 2, and the minimum inhibitory concentrations were either similar to or lower than that of kanamycin. These results suggest that the peel and seeds of camu-camu fruit could be utilized for therapeutic applications. 相似文献
18.
Ssanghwa-tang is a medicinal formula that is widely prescribed in Korea to decrease fatigue after an illness. Fermented herbal
medicines might be made more efficacious than conventional herbal medicines by increasing the absorption and bioavailability
of the active compounds. In this study, Ssanghwa-tang was fermented to produce bioconversion compositions using Lactobacillus fermentum, and six peaks were decreased, four peaks were increased and one peak newly appeared in the HPLC-DAD chromatogram. The structures
of the newly-appearing compound (1) and increased (2–5) compounds were identified as follows using NMR and MS: liquiritigenin (1), nodakenetin (2), cinnamyl alcohol (3), decursinol (4), and benzoic acid (5). The decreased compounds were identified to be paeoniflorin (6), liquiritin (7), nodakenin (8), cinnamaldehyde (9), decursin (10), and decursinol angelate (11) using HPLC-DAD analysis with authentic compounds. The high performance liquid chromatography method was used to quantify
the eleven constituents in Ssanghwa-tang and fermented Ssanghwa-tang. All calibration curves of the standard compounds exhibited
excellent linearity with a R2 > 0.9940. 相似文献
19.
M. R. Aouad 《Nucleosides, nucleotides & nucleic acids》2016,35(1):1-15
The solvent-free 1,3-dipolar cycloaddition reaction of dimethylacetylene dicarboxylate (1) with 2-chlorophenyl azide (2) afforded 1,2,3-triazole diester 3 that upon hydrazinolysis, furnished the corresponding bis-acid hydrazide 4. The treatment of compound 4 with carbon disulfide in a refluxing potassium hydroxide solution furnished the desired bis-1,3,4-oxadiazole-2-thione 5 tethered to a 1,2,3-triazole moiety. The respective SOx-glycosides 9–11 were obtained by glycosylation of bis-oxadiazole 5 with 2,3,4,6-tetra-O-acetyl-α-d-glucopyranosyl bromide (6), 2,3,4,6-tetra-O-acetyl-α-d-galactopyranosyl bromide (7), and 2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-α-d-glucopyranosyl chloride (8) in dry acetone in the presence of Et3N, which acted as a base. However, alkylation of 5 with halogeno-alkanol 12 or 13, chloroglycerol 14, bromoethers 20 or 21, and epichlohydrin 22 in the presence of K2CO3 in DMF yielded the corresponding acyclonucleoside analogs 16–18 and 23–25. The isopropylidenes 19 and acetyl derivatives 26–28 of the products were also prepared. The newly synthesized compounds were characterized by 1H NMR, 13C NMR, 2D NMR, and mass spectra. The compounds were screened for their antibacterial and antifungal activities. A number of the tested compounds exhibited significant antimicrobial activity compared to the reference drugs. 相似文献
20.
Natália Alvarenga 《Biocatalysis and Biotransformation》2017,35(6):388-396
Several marine-derived fungi were evaluated by the bioreduction of 2-azido-1-phenylethanone 1, and the strains A. sydowii CBMAI 935 and M. racemosus CBMAI 847 were selected for the reduction of 2-azido-1-phenylethanone derivatives 2–4. Whole cells of A. sydowii CBMAI 935 promoted the reduction of 2-azido-1-phenylethanones 1–4 with high selectivities to yield the (S)-2-azido-1-phenylethanols 1a–4a. Bioreduction of compounds 1–4 by M. racemosus CBMAI 847 led to (R)-2-azido-1-phenylethanols for 1, 2 and 4 and (S)-2-azido-1-phenylethanol 3. Enantiomerically enriched 2-azido-1-phenylethanols 1a–4a and phenylacetylene 5 were applied in the synthesis of β-hydroxy-1,2,3-triazoles using CuSO4 and sodium ascorbate leading to regioselective formation of enantioenriched 1,4-disubstituted 1,2,3-triazole compounds 1b–4b. 相似文献