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  • lead compounds
  • The anti-MRSA activity of compounds 21 (MIC ¼ 3.9 mg/mL, MBC ¼ 7.8 mg/mL) and 22 (MIC ¼ 1.95 mg/mL, MBC ¼ 7.8 mg/mL) was significantly greater than that of the lead compounds, 1e3 and reference antibiotics penicillin G (MIC ¼ 31.25 mg/mL) and ciprofloxacin (MIC ¼ 7.8 mg/mL) and comparable to that of vancomycin (MIC ¼ 0.97 mg/mL). (scribd.com)
  • From a set of weakly potent lead compounds, using in silico screening and small library synthesis, a series of 2-alkyl-3-aryl-3-alkoxyisoindolinones has been identified as inhibitors of the MDM2-p53 interaction. (ox.ac.uk)
  • extract
  • Fractionation of ethanol extract of fruits yielded 18 compounds[ 12 were elucidated as Ethyl 3,4,5-Trihdroxybenzoate (1)、4-ethylgallic acid (2)、Hydroxyhydroquinone (3)、Gallic acid (4)、β-Sitosterol (5)、β-Daucosterol (6)、Stigmasterol (7)、Protocatechuic acid (8)、Palmitic acid (9)、Linoleic acid (10)、Cis-Oleic acid (11)、5-hydroxymethyl-2-Furancarboxaldehyde (12). (stuartxchange.com)
  • Fractionation of a petroleum ether extract yielded 29 compounds, amounting to 69.67% of the total detected constituents. (stuartxchange.com)
  • The application of this technique to stepwise diluted extracts of the volatile compounds allowed the determination of a new parameter, the D -value, which reveals the most intense flavour compounds of an extract. (springer.com)
  • selectivity
  • Harrisonia perforata was one of six plants with possible novel antimalarial compounds, with antiplasmodial activity (IC50 ranging from 0.4 to 8.6 mu g/ml) with good selectivity. (stuartxchange.com)
  • Furthermore, the cytotoxicity of (-)mycousnine enamine was lower than that of cyclosporin A, and its therapeutic index (TC50/EC50) was 4,463.5, which is five-fold higher than that of cyclosporin A. We conclude that (-)mycousnine enamine (2), the semi-synthestic product prepared from the native product (-)mycousnine (1) of the endophyte M. nawae is a novel effective immunosuppressant showing low toxicity and high selectivity. (frontiersin.org)
  • Compound 29 has been tested in the Ambit 442 kinase panel and demonstrates good selectivity for the Pim kinase family. (sigmaaldrich.com)
  • potency
  • A dual orexin receptor antagonist (DORA), almorexant (ACT-078573), blocks both OX 1 R and OX 2 R with similar potency (IC 50 16 and 15 nM, respectively). (frontiersin.org)
  • Oleocanthal is a natural inflammation-fighting compound with potency strikingly similar to that of the drug ibuprofen in inhibiting an enzyme that causes pain and inflammation. (care2.com)
  • chemical
  • We describe here the total chemical synthesis of the trisaccharide GlcNS6S-GlcA-1,6anGlcNS ( 1 ) and its glycol-split (gs) counterpart GlcNS6S-gsGlcA-1,6anGlcNS ( 2 ) from glucose. (mdpi.com)
  • ethyl
  • Study of fruit isolated 8 compounds: caryolane-1,9beta-diol (1), gallic acid (2), 4-O-ethylgallic acid (3), syringic acid ethyl ester (4), protocatechuic acid (5), stigmasterol (6), beta-daucoster (7), beta-sitosterol (8). (stuartxchange.com)
  • Arrest
  • It inhibited microtubule assembly followed by M-phase arrest, Bcl-2 inactivation, and then apoptosis through caspase pathways. (aacrjournals.org)
  • series
  • A series of these compounds was synthesized and assayed against purified nNOS enzymes, endothelial NOS (eNOS), and inducible NOS (iNOS). (rcsb.org)
  • results
  • Together, these results suggest that an orexin-mediated suppression of REM sleep via potential activation of OX 1 Rs in the locus coeruleus may possibly contribute to the differential effects on sleep/wakefulness exerted by a DORA as compared to a 2-SORA. (frontiersin.org)
  • Overall, the results suggest that compounds 21 and 22 may be of potential use in the treatment of MRSA infections. (scribd.com)
  • small
  • Nickel is also a naturally magnetostrictive material, meaning that in the presence of a magnetic field, the material undergoes a small change in length (2). (thefreelibrary.com)
  • These data represent a detailed examination of the action of different flavonoids on peptide agonists at the GLP-1R and may aid in the development of future small molecule compounds targeted at this receptor. (aspetjournals.org)
  • cells
  • The major function of microtubules is to partition the duplicate chromosomes equally into the daughter cells through spindle formation during the mitosis of cell cycle ( 1 , 2 ). (aacrjournals.org)
  • In malignant cells, this process is essential for tumor growth and the dynamics of the tubulin-microtubule cycle speeds up in cell dividing ( 2 - 5 ). (aacrjournals.org)
  • values
  • Hexanal, 2(Z)-octenal and 2(E)-nonenal exhibited the highest D -values in both lipids. (springer.com)
  • After 48 h aldehyde and hexanal and after 72 h hexanal and 2(Z)-octenal possessed the highest D -values. (springer.com)
  • The D -value can also be used for the approximation of odour threshold values as demonstrated for 2(Z)-octenal, 2(E)-nonenal and 1-octen-3-ol. (springer.com)
  • cancer
  • Since pomegranates have anti-inflammatory attributes, they are perfect for lowering inflammation, helping to avoid type 2 diabetes, cancer, heart disease, obesity and Alzheimer's disease. (blogspot.com)
  • Study
  • According to one study, people with high blood pressure have drastically lowered their blood pressure in a period of 2 weeks, with a daily consumption of 150 ml of pomegranate juice. (blogspot.com)
  • Study yielded eight limonoids (1-8) including three A, B and D-seco-16-nor-type ones, 5,6-dehydrodesepoxyharperforin C2 (1), harrpernoid B (2), and its C-9S epimer, harrpernoid C (3), along with six known compounds (9-14), were isolated from fruits of Harrisonia perforata. (stuartxchange.com)
  • We have established the first model to study deficiency of mitochondrial thymidine kinase 2 (TK2) by creating a strain of TK2 knock-out mice. (ki.se)
  • response
  • Although insulin release downstream of GLP-1R activation is known to be critically dependent upon the formation of cAMP, there is also a role for mobilization of intracellular Ca 2+ and activation of mitogen-activated protein kinases such as extracellular signal-regulated kinase 1 and 2 (ERK1/2) in augmentation of insulin response ( Baggio and Drucker, 2007 ). (aspetjournals.org)