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11.
From the roots of oat (Avena sativa) a second antibiotic active glycoside, avenacine B, was isolated in addition to the main glycoside avenacine A. In the aglycone of A the double bond could not be established contrary to the statement in the literature but an aldehyde group in addition to the keto group was identified and therefore the proposed structure has to be revised. In the aglycone of B the —CH2OH-group of A has been substituted by CH3. The structures of the sugar chains in both glycosides have been determined, in avenacine A as [β-d-gluco-pyranosyl(1 → 4)-[β-d-glucopyranosyl (1 → 2)]-α-l-arabinosyl (1)- and in B as [β-d-glucopyranosyl (1 → 4)]-β-d-glucopyranosyl (1)-. 相似文献
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14.
Dr. Jakov Ivkovic Dr. Shalinee Jha Dipl.-Ing. Christian Lembacher-Fadum Dipl.-Ing. Johannes Puschnig Dr. Prashant Kumar Dr. Viktoria Reithofer Prof. Dr. Karl Gruber Prof. Dr. Peter Macheroux Prof. Dr. Rolf Breinbauer 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(56):14108-14120
Dipeptidyl peptidase III (DPP3) is a ubiquitously expressed Zn-dependent protease, which plays an important role in regulating endogenous peptide hormones, such as enkephalins or angiotensins. In previous biophysical studies, it could be shown that substrate binding is driven by a large entropic contribution due to the release of water molecules from the closing binding cleft. Here, the design, synthesis and biophysical characterization of peptidomimetic inhibitors is reported, using for the first time an hydroxyethylene transition-state mimetic for a metalloprotease. Efficient routes for the synthesis of both stereoisomers of the pseudopeptide core were developed, which allowed the synthesis of peptidomimetic inhibitors mimicking the VVYPW-motif of tynorphin. The best inhibitors inhibit DPP3 in the low μM range. Biophysical characterization by means of ITC measurement and X-ray crystallography confirm the unusual entropy-driven mode of binding. Stability assays demonstrated the desired stability of these inhibitors, which efficiently inhibited DPP3 in mouse brain homogenate. 相似文献
15.
Physics of the Solid State - Polycrystalline samples of La0.67Sr0.33Mn0.65Fe0.35O3 (LSMFO) were synthesized using the standard ball mill method with different calcination temperatures ranging from... 相似文献
16.
Acid catalysed epoxy ring opening of several lupane type triterpenoids leads to unusual allylic hydroxylation. The reaction involves the formation of epoxide by m‐chloroperbenzoic acid followed by the treatment of mineral acid. The simple methodology finds utility to introduce a hydroxyl function at the allylic position in these triterpenoids, which is otherwise quite difficult. 相似文献
17.
Sonika Pandey Avinash Mishra Manish Kumar Patel Bhavanath Jha 《Applied biochemistry and biotechnology》2013,171(1):1-9
Cumin is an annual herbaceous medicinally important plant having diverse applications. An efficient and reproducible method of Agrobacterium-mediated genetic transformation was herein established for the first time. A direct regeneration method without callus induction was optimised using embryos as explant material in Gamborg’s B5 medium supplemented with 0.5-μM 6-benzyladenine and 2.0-μM α-naphthalene acetic acid. About 1,020 embryos (a mean of 255 embryos per batch) were used for the optimisation of transformation conditions. These conditions were an Agrobacterium cell suspension of 0.6 OD600, a co-cultivation time of 72 h, 300-μM acetosyringone and wounding of explants using a razor blade. Pre-cultured elongated embryos were treated using optimised conditions. About 720 embryos (a mean of 180 embryos per batch) were used for transformation and 95 % embryos showed transient β-glucuronidase expression after co-cultivation. Putative transformed embryos were cultured on B5 medium for shoot proliferation and 21 regenerated plants were obtained after selection and allowed to root. T0 plantlets showed β-glucuronidase expression and gene integration was confirmed via PCR amplification of 0.96 and 1.28 kb fragments of the hygromycin-phosphotransferase II and β-glucuronidase genes, respectively. In this study, a transformation efficiency of 1.5 % was demonstrated and a total of 11 transgenic plants were obtained at the hardening stage, however, only four plants acclimatised during hardening. Gene copy number was analysed by Southern blot analysis of hardened plants and single-copy gene integration was observed. This is the first successful attempt of Agrobacterium-mediated genetic transformation of cumin. 相似文献
18.
A tandem approach for the regio- and stereoselective synthesis of oxazolo-fused pyrroloquinolines 3a–l via the reaction of o-alkynylaldehydes 1a–i with chiral amino alcohols 2a–c under mild reaction conditions is described. The possible participation of the pyridine ring in the regioselective formation of 5-exo-dig cyclized products was supported by the controlled experiments. The structures and stereochemistry of the products were confirmed by NOESY and X-ray crystallographic studies. 相似文献
19.
Durga Charan Panigrahi Patitapaban Sahu Devi Prasad Mishra Vivekanand Jha R. Lokeswara Patnaik 《Journal of Radioanalytical and Nuclear Chemistry》2014,302(1):433-439
This paper presents the assessment of inhalation exposure potential of broken uranium ore piles in different stopes of Jaduguda uranium mines of India. 222Rn emanation coefficient of broken uranium ore was measured in laboratory by collecting air sample from airtight glass jar containing ore sample. An attempt was also made to correlate the emanation coefficient with 226Ra content of the ore. The 222Rn progeny doses estimated based on radon activity concentration of broken ore, occupancy period and equilibrium ratio in different stopes were well below the prescribed limit of International Commission on Radiological Protection. The maximum 222Rn progeny dose contribution from broken ore piles was worked out to be 0.22 mSv year?1. This suggests that the broken ore piles are not the significant contributor of inhalation exposure under the existing ventilation condition of Jaduguda uranium mine. 相似文献
20.
In the present article, a dataset of 63 quinoxaline derivatives were taken for antimalarial activity and pharmacophore were developed. Atom based method was used to develop a three dimensional quantitative structure activity relationship (3D-QSAR) model. On comparison of all statistical parameters, model AHRRR23 was found to be the most effective and predictive QSAR model as it satisfied all statistical parameters of a good model. The model AHRRR23 showed an adequate R2 value for the training set 0.9446, good predictive power with Q2 of 0.6409, good F- value, low SD 0.1218 value and outstanding Pearson-R values and low RMSE 0.2779 values of the model. The docking studies also gives very good results with good RMSD values. 3D QSAR, docking and ADME studies exhibits that the developed model could be employed as a potential lead for further study as antimalarial drug. 相似文献