共查询到20条相似文献,搜索用时 15 毫秒
1.
Yoshihiro Nishida Hiroshi Ohrui Hiroshi Meguro 《Bioscience, biotechnology, and biochemistry》2013,77(5):1217-1221
(+)-Marmelo oxide A and (—)-marmelo oxide B were stereoselectively synthesized from d-glutamic acid via (—)-marmelo lactones A and B. The absolute configurations of marmleo oxides were thus determined to be the (+)-oxide A having the (2R, 4R) and (+)-oxide B having (2S, 4R) configurations. 相似文献
2.
Sung-Jae Lee Won-Hwan Park Sun-Dong Park 《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):957-959
Diabetes is one of the major risk factors for cataract. Aldose reductase has been reported to play an important role in sugar-induced cataract. In this study, we conducted pharmacological investigations upon experimental rat lenses using extracts of the fruits of Litchi chinensis (Sapindaceae). Of the extracts and organic fractions of L. chinensis tested, a MeOH extract and an EtOAc fraction were found to be potent inhibitors of rat lens aldose reductase (RLAR) in vitro — their IC50 values being 3.6 and 0.3 μg/mL, respectively. From the active EtOAc fraction, four minor compounds with diverse structural moieties were isolated and identified as d-mannitol (1), 2,5-dihydroxybenzoic acid (2), delphinidin 3-O-β-galactopyranoside-39,59-di-O-β-glucopyranoside (3), and delphinidin 3-O-β- galactopyranoside-39-O-β-glucopyranoside (4). Among these, 4 was found to be the most potent RLAR inhibitor (IC50 = 0.23 μg/mL), and may be useful in the prevention and/or treatment of diabetic complications. 相似文献
3.
A. K. Das M. Ghosh A. K. Basak S. K. Mazumdar R. A. Palmer 《Nucleosides, nucleotides & nucleic acids》2013,32(5):731-744
Abstract 1–C3′, 3′, 5′–Tri—O—acetyl— β—D—ribof uranosyll)—3—acetoxy —2—pyridone,crystallised in space group P2 with z=2 and cell parameters a=12. 446(2), b=10. 415(2), c=7. 600(2) A, β=03. 3O(4). The structure was solved by direct methods and refined by full—matrix least—squares to a final R value of 0·251 for 1847 observed reflections. The sugar—pucker is found to be 3ECC3′ endo) with P = 17.7° and xCN=170. 2(2)° in the range. The C4′-C5′ conformation is gauche minus. Because of the absence of H—bond donor atoms. the crystal structure is stabilised by a network of C-H—-O close contacts. No base stacking is observed. 相似文献
4.
N.A. Martin 《New Zealand journal of zoology.》2013,40(1):121-155
Abstract Six species of Siteroptes subgenus Siteroptoides—kneeboni (Wicht), mesembrinae (Canestrini), microsaniae n.sp., morelliae (Rack), muscarius n.sp., and portatus n.sp.—have been found in New Zealand. S. (S.) mesembrinae occurs on Niue Island also, and a further new species, pacificus, is recorded from Tonga. The phoretomorph females of all 7 species, the normal females of 4, the males of 3, and larvae of 2 are described and compared. The similarities and differences between normal and phoretomorph females are particularly noted. Besides kneeboni, 2 species described by Wicht but not occuring in New Zealand—athiasae and flechtmanni— are redescribed from type material and transferred to Siteroptes (Siteroptoides). Keys are given for normal females and Pediculaster-like phoretomorph females of Siteroptoides. Siteroptes mesembrinae subsimilis and S. ignotus altaicus are raised to species status. Diagnostically important measurements are given to help define the variation within and between species and morphs. 相似文献
5.
Leucaspis gigas (Maskell, 1879) and 3 other endemic species which have been confused with it— L. ohakunensis Brittin, L. morrisi (Brittin), and Salicicola maskelli (Brittin)—are redescribed; L. mixta de Boer, also endemic, is described as new. All species are illustrated. Lectotypes are designated where appropriate. 相似文献
6.
Jiro Yamada 《Bioscience, biotechnology, and biochemistry》2013,77(4):997-999
Valsa ceratosperma, which is the pathogenic fungus of apple canker, was grown in a synthetic medium. The neutral extract from the culture filtrate was chromatographed on a silica gel column to give five isocoumarins. Their structures were determined by MS, UV, IR, 1H and 13C NMR, and CD spectra. Three of them were known compounds; ( ? )-5-methylmellein (1), ( ? )-5-carboxylmellein (2) and ( ? )-5-hydroxylmethylmellein (3). Since the absolute configurations at C-3 in 2 and 3 were not known until now, both were determined to be R by chemical correlations. The two were new compounds; ( + )-(3R,4S)-trans-4-hydroxy-5-methylmellein (4) and ( ? )-(3R,4R)-cis-4-hydroxy-5-methylmellein (5). All the five compounds showed phytotoxicity in a bioassay using detached apple shoots and lettuce seedlings. 相似文献
7.
Hinako Shirakata Hisashi Nishiwaki 《Bioscience, biotechnology, and biochemistry》2020,84(10):1986-1996
ABSTRACT All eight stereoisomers of conidendrin were synthesized from (1 R,2 S,3 S)-1-(4-benzyloxy-3-methoxyphenyl)-3-(4-benzyloxy-3-methoxybenzyl)-2- hydroxymethyl-1,4-butanediol ((+)-4) and its enantiomer with high optical purity. The configurations at 4-positions of the conidendrin stereoisomers were constructed by intramolecular Friedel-Crafts reaction of protected 4. After conversion to tetrahydronaphthalene intermediate 7a, the 2- and 3-position of tetrahydronaphthalene structure 7a were converted to 3a- and 9a-position of (+)-α-conidendrin (3a), respectively. By the epimerization process of 2- or 3-position of 7a, the other diastereomers were obtained. All enantiomers were also synthesized from (?)-4. 相似文献
8.
9.
Darren Griffith Sara Cecco Ennio Zangrando Alberta Bergamo Gianni Sava Celine J. Marmion 《Journal of biological inorganic chemistry》2008,13(4):511-520
Reaction of 3-pyridinehydroxamic acid and 4-pyridinehydroxamic acid (3-pyha and 4-pyha) with either [NBu4][RuCl4(dmso-S)2] or [(dmso)2H][RuCl4(dmso-S)2] (dmso is dimethyl sulfoxide) in acetone afforded three new ruthenium(III) dimethyl sulfoxide pyridinehydroxamic acid complexes:
[NBu4][trans-RuCl4(dmso-S)(4-pyha)]·CH3COCH3 (1), [3-pyhaH][trans-RuCl4(dmso-S)(3-pyha)] (2) and [4-pyhaH][trans-RuCl4(dmso-S)(4-pyha)] (3). The solid-state structure of [NBu4][trans-RuCl4(dmso-S)(4-pyha)]·CH3COCH3 (1) was determined by X-ray crystallography. 2 and 3 were pharmacologically evaluated for their in vitro cytotoxicity, their ability to inhibit cell invasion and their gelatinase
activity. 2 and 3 were devoid of cytotoxicity against the cell lines tested. 2 inhibited invasion of the highly invasive MDA-MB-231 cells to a much greater extent than 3. Contrary to expectations, neither 2 nor 3 had any inhibitory effect on matrix metalloproteinase (MMP) production and/or activity and in fact 3 was found to enhance the production and/or activity of both MMP-2 and MMP-9. 相似文献
10.
As part of an effort to generate broad-spectrum inhibitors of rhinovirus replication, novel series of (E)-3-[(E)-3-phenylallylidene]chroman-4-ones 1a–e, (E)-3-(3-phenylprop-2-yn-1-ylidene)chroman-4-ones 2a and 2b, (Z)-3-[(E)-3-phenylallylidene]chromans 3a–e, and (E)-3-(3-phenylprop-1-en-1-yl)-2H-chromenes 4a–d were designed and synthesized. All the compounds were tested in vitro for their efficacy against infection by human rhinovirus (HRV) 1B and 14, two representative serotypes for rhinovirus group B and A, respectively. Most of the analogues were found to be potent and selective inhibitors of both HRVs, although HRV 1B was generally more susceptible than HRV 14. Mechanism of action studies of (E)-6-chloro-3-(3-phenylprop-1-en-1-yl)-2H-chromene 4b, the most potent compound on HRV 1B infection, suggested that 4b behaves as a capsid-binder probably acting at the uncoating level. 相似文献
11.
Marzena Rządkowska Elżbieta Szacoń Agnieszka A. Kaczor Barbara Rajtar Łukasz Świątek Małgorzata Polz-Dacewicz 《Journal of enzyme inhibition and medicinal chemistry》2016,31(5):787-795
Novel 1-(1-aryl-4,5dihydro-1H-imidazoline)-3-chlorosulfonylourea derivatives 3a–3f were synthesized in the reaction of 1-aryl-4,5-dihydro-1H-imidazol-2-amines with chlorosulfonyl isocyanate. The second series of compounds 4a–4f was prepared from the respective 1-(1-aryl-4,5-dihydro-1H-imidazoline)-3-chlorsulfonylureas 3a–3f and 1,1′-carbonyldiimidazole (CDI). The selected compounds were tested for their activity against Herpes simplex virus and coxsackievirus B3 (CVB3). It was determined that three derivatives, i.e 3d, 4a and 4d are active against Herpes simplex virus (HSV-1). Compounds 3d and 4c are active against CVB3. Their favorable activity can be primarily attributed to their low lipophilicity values. Moreover, the lack of substituent in the phenyl moiety or 4-methoxy substitution can be considered as the most beneficial for the antiviral activity. 相似文献
12.
《Journal of enzyme inhibition and medicinal chemistry》2013,28(5):968-973
In this work, we reported the synthesis and evaluation of antibacterial and antifungal activities of three new compound series obtained from 6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazole-3-acetic acid hydrazide: 2-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl}-N-alkyl/arylhydrazinecarbothioamides (2a–d), 4-alkyl/aryl-2,4-dihydro-5-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]methyl}-3H-1,2,4-triazole-3-thiones (3a–n), and 2-alkyl/arylamino-5-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]methyl}-1,3,4-thiadiazoles (4a–g). The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR (APT), mass and elemental analysis. Their antibacterial and antifungal activities were evaluated against Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Candida albicans ATCC 10231, C. parapsilosis ATCC 22019, C. krusei ATCC 6258, Trichophyton mentagrophytes var. erinacei NCPF 375, Microsporum gypseum NCPF 580, and T. tonsurans NCPF 245. 3c, 3f, 3m, 3n, and 4e showed the highest antibacterial activity. Particularly 3c, 3f, 3g, 3k, 3n, 4a, 4e, and 4g showed the highest antifungal activity against tested fungi. 相似文献
13.
为了解柯拉斯那(Aquilaria crassna)的化学成分,从其所产沉香中分离得到10个化合物,经波谱分析分别鉴定为:6,8-羟基-2-(2-苯乙基)色酮(1),6,8-二羟基-2-[2-(4-甲氧基苯)乙基]色酮(2),rel-(1a R,2R,3R,7b S)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-5-(2-phenylethyl)-7H-oxireno[f][1]benzopyran-7-one(3),rel-(1a R,2R,3R,7b S)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-[2-(4-methoxyphenyl)-ethyl]-7H-oxireno[f][1]benzopyran-7-one(4),rel-(1a R,2R,3R,7b S)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-5-[2-(3-hydroxy-4-methoxyphenyl)-ethyl]-7H-oxireno[f][1]benzopyran-7-one(5),oxidoagarochromone B(6),oxidoagarochromone C(7),(5S,6R,7S,8R)-2-[2-(3′-hydroxy-4′-methoxyphenyl)ethyl]-5,6,7,8-tetrahydroxy-5,6,7,8-tetrahydrochromone(8),6,7-cis-dihydroxy-2-(2-phenylethyl)-5,6,7,8-tetrahydrochromone(9),N-trans-feruloyltyramine(10)。化合物3~5和8~10为首次从柯拉斯那沉香中分离得到。化合物1,3,6,7,9和10对乙酰胆碱酯酶具有一定的抑制活性,化合物4对人慢性髓原白血病细胞株K-562和人胃癌细胞株SGC-7901均具有较小的抑制作用,化合物1和3对人肝癌细胞株BEL-7402也有抑制活性。 相似文献
14.
Zahid Mozaffar Kazuhiro Nakanishi Ryuichi Matsuno Tadashi Kamikubo 《Bioscience, biotechnology, and biochemistry》2013,77(12):3053-3061
Six compounds, Z- and E-fadyenolide (3, 4), 1-ally1-2,3-(methylenedioxy)-4,5-dimethoxy-benzene (5), 4-methoxy-3,5-bis (3′-methyl-2′-butenyl)-benzoic acid (6), 2,6-dihydroxy-4-methoxy-dihydrochalcone (7), and 5-hydroxy-7-methoxyflavanone (8) were isolated from three species of Jamaican Piper, Piper fadyenii, C.D.C., Piper aduncum L. and Piper hispidum Sw. Three amides (9 ~ 11) of 3,5-dimethoxy-4-oxo-5-phenylpent-2-enoic acid using piperidine, pyrrolidine and morpholine, respectively, were synthesized from compounds 3 and 4, and tested for insecticidal activity against the tick Boophilus microplus (Canestrini) and the flour feetle, Tribolium confusum Duval. In our experiment, compounds 9 ~ 11 inhibited ovogenesis of B. microplus and were toxic to T. confusum. Compounds 3 ~ 8 were found to have no activity. 相似文献
15.
《Journal of enzyme inhibition and medicinal chemistry》2013,28(1):126-131
Novel 1-[[4-(4-bromophenyl)-5-(2-furyl)-4H-1,2,4-triazole-3-yl]mercaptoacetyl]-4-alkyl/aryl-3-thiosemicarbazides (5–12) were synthesized by the reaction of 4-(4-bromophenyl)-5-(2-furyl)-4H-1,2,4-triazole-3-ylmercaptoacetylhydrazide (4) with substituted isothiocyanates. Cyclodehydration of thiosemicarbazides with concentrated sulfuric acid yielded 2-[4-(4-bromophenyl)-5-(2-furyl)-4H-1,2,4-triazole-3-yl]mercaptomethyl-5-alkyl/arylamino-1,3, 4-thiadiazoles (13–17). The new compounds were evaluated for in vitro antifungal activity using the microdilution method. The tested compounds showed varying degrees of activity against Microsporum gypseum NCPF-580, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum, and Candida albicans ATCC 10231 (MIC 8–4 μg/mL). 相似文献
16.
Phytochemical investigation of the underground parts of Liriope graminifolia (Linn.) Baker resulted in the isolation of two new steroidal saponins lirigramosides A (1) and B (2) along with four known compounds. The structures were determined by extensive spectral analysis, including two-dimensional (2D) NMR spectroscopy and chemical methods, to be 3-O-{β-d-xylopyranosyl-(1→3)-α-l-arabinopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→4)]-β-d-glucopyranosyl-(25S)-spirost-5-ene-3β,17α-diol (1), 1-O-[α-l-rhamnopyranosyl-(1→2)-β-d-xylopyranosyl]-(25R)-ruscogenin (2), 1-O-β-d-xylopyranosyl-3-O-α-l-rhamnopyranosyl-(25S)-ruscogenin (3), 3-O-α-l-rhamnopyranosyl-1-O-sulfo-(25S)-ruscogenin (4), methylophiopogonanone B (5), and 5,7-dihydroxy-3-(4-methoxybenzyl)-6-methyl-chroman-4-one, (ophiopogonanone B, 6), respectively. Compound 1 has a new (25S)-spirost-5-ene-3β,17α-diol ((25S)-pennogenin) aglycone moiety. The isolated compounds were evaluated for their cytotoxic activities against Hela and SMMC-7721 cells. 相似文献
17.
《Nucleosides, nucleotides & nucleic acids》2013,32(4-7):879-882
The thioamide derivatives 3′-deoxy-5′-O-(4,4′-dimethoxytrityl)-3′-[(2-methyl-1-thioxo-propyl)amino]thymidine 1 and 3′-deoxy-5′-O-(4,4′-dimethoxytrityl)-3′-{{6-{[(9H-(fluo-ren-9-ylmethoxy)carbonyl]-amino}-1-thioxohexyl}amino} thymidine 2 were synthesized by regioselective thionation of their corresponding amides 7 and 8 with 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphet-ane-2,4-disulfide (Lawesson's reagent). The thioamides were converted into the corresponding 5′-triphosphates 3 and 4. Compound 3 was chosen for DNA sequencing experiments and 4 was further labelled with fluorescein. 相似文献
18.
《Biotechnic & histochemistry》2013,88(4):199-200
Lipp, Walther. Histochemische Methoden. About 24 pages per issue; 3 issues (No. 9, 10 and 11) during 1956. 16 £ 23 cm. R. Oldenbourg, München 1, Germany. DM 30.—for 6 issues; DM 6.—per single copy. (In German)Molenaar, I. Ontkalking van harde weefsals. Een histochemische studie. Thesis, Rijksuniversiteit te Utrecht, 1957. pp. 124. 相似文献
19.
Sensilla on the antennae of 5 species of hepialid moths—Aenetus virescens (Hepialinae) and Wiseana cervinata, W. signata, W. umbraculata, and Trioxycanus enysii (Oxycaninae)—were examined with the scanning electron microscope. Only 4 of the 6 types of sensilla previously described from noctuid moths were observed. The arrays of sensilla on oxycanine species are not uniformly distributed, especially on males; most of the sensors on any segment are on the ‘ridge’ of the pectinations, with a sparse distribution of relatively widely spaced sensors on the rest of the cuticle. In all species examined the antennae were sexually dimorphic; this was most apparent in the differing sensilla arrays of Hepialinae and in the difference in size of the antennal pectinations of Oxycaninae. 相似文献
20.
(±)-(2Z,4E)-α-Ionylideneacetic acid (2) was enantioselectively oxidized to (?)-(l′S)-(2Z,4E)-4′-hydroxy-α-ionylideneacetic acid (3), (+)-(1′R)-(2Z,4E)-4′-oxo-α-ionylideneacetic acid (4) and (+)-abscisic acid (ABA) (1) by Cercospora cruenta IFO 6164, which can produce (+)-ABA and (+)-4′-oxo-α-acid 4. This metabolism was confirmed by the incorporation of radioactivity from (±)-(2-14C)-(2Z,4E)-α-acid 2 into three metabolites. (?)-4′-Hydroxy-α-acid 3 was a diastereoisomeric mixture consisting of major 1′,4′-trance-4′-hydroxy-α-acid 3a and minor 1′,4′-cis-4′-hydroxy-α-acid 3b. These structures, 3a and 3b, were confirmed by 13C-NMR and 1H-NMR analysis. Also, the enantioselectivity of the microbial oxidation was reexamined by using optically pure α-acid (+)-2 and (?)-2, as the substrates. 相似文献