73022-40-9Relevant academic research and scientific papers
Using fluorogenic probes for the investigation of selective biomass degradation by fungi
Zhang, Qian,Peng, Xinrui,Grilley, Michelle,Takemoto, Jon Y.,Chang, Cheng-Wei Tom
, p. 1918 - 1925 (2015/03/18)
A library of fifteen commercially purchased and synthetic fluorogenic probes was employed for the investigation of biomass degradation using extracts of white-rot fungi. These probes were selected or designed to mimic the dominant linkages in celluloses, hemicelluloses, and lignin, the three most abundant polymers found in biomass. The results show that white-rot fungi display a high preference for cleaving mannose- and glucose-based probes, which mimic hemicelluloses. Low degrees of cleavages were noted for xylose- and cellobiose-based probes. No cleavages were observed for probes that mimic the linkages in lignin. Overall, these discoveries prove that it is possible to employ fungi for selective degradation or release of hemicelluloses from biomass.
Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models
H?gmoen ?strand, Ove Alexander,Gikling, Ingvei,Sylte, Ingebrigt,Rustan, Arild Christian,Thoresen, G. Hege,Rongved, P?l,Kase, Eili Tranheim
, p. 258 - 263 (2014/02/14)
Four new mimics of 22-S-hydroxycholesterol (22SHC) were synthesized and evaluated using molecular modeling and tested in human muscle cells (primary myotubes) and hepatocytes (HepG2 cells). The new compounds (9, 12, 15a and 15b) showed good interrelationship between docking scores, to both LXRα and LXRβ, and in vitro results. The LXR agonist T0901317 increased the expressions of genes involved in lipogenesis (SCD1, FAS) and cholesterol efflux (ABCA1), but only 22SHC counteracted the up-regulation of SCD1 and FAS by T0901317. Compound 9 and 12 decreased the expression of SCD1, while 9 also decreased the expression of FAS. Compounds 15a showed a significant antagonistic effect on ABCA1 expression, but neither 15a nor 15b were able to counteract the effect of T0901317 on all genes examined. Lipogenesis was increased after T0901317 treatment and only 22SHC significantly counteracted this effect. Treatment with 22SHC and compound 12 reduced lipogenesis compared to control. An increased glucose uptake was observed for all compounds, except for 15b. In summary, the new synthetic 22SHC mimics showed antagonistic effects similar to that of 22SHC, but the new substances were less potent. The sulfonamide 12 showed similar effects to 22SHC and the best effect on gene expression of the new mimics, however, it was not able to reduce the effect of T0901317 as observed for 22SHC.
NAPTHTHALENE DERIVATIVES WHICH INHIBIT THE CYTOKINE OR BIOLOGICAL ACTIVITY OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)
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Page 88, (2010/02/04)
Where Y, R1-R8 and R101-R108 are as defined in the specification. Compounds of formula (II) and methods of inhibiting the cytokine or biological activity of Macrophage Migrating Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy.
Enantioselective hydrolysis of naproxen ethyl ester catalyzed by monoclonal antibodies
Shi, Zhen-Dan,Yang, Bing-Hui,Zhao, Jing-Jing,Wu, Yu-Lin,Ji, Yong-Yong,Yeh, Ming
, p. 2171 - 2175 (2007/10/03)
This report described that a hapten of racemic phosphonate 3 designed as the mimic of the transition state of hydrolysis of naproxen ethyl ester was successfully synthesized from easily available 2-acetyl-6-methoxy-naphthalene 5. Then BALB/C mice were immunized and one of the monoclonal catalytic antibodies, N116-27, which enantioselectively accelerated the hydrolysis of the R-(-)-naproxen ethyl ester was given. The Michaelis-Menton parameter for the catalyzed reaction was KM=6.67 mM and kcat/kuncat=5.8×104. This enantioselective result was explained by the fact that the R-isomer of rac-hapten was more immunogenic than the S-isomer.
Synthesis of suspected carcinogenic metabolites of 7H-benzo[c]fluorene, a coal tar component implicated in causation of lung tumors.
Wang, Ji-Quan,Weyand, Eric H,Harvey, Ronald G
, p. 6216 - 6219 (2007/10/03)
High incidences of lung tumors were observed in mice fed coal tar in their diet. The principal component of tar that gives rise to DNA-bound adducts in mouse lung was identified as 7H-benzo[c]fluorene (BcF). We now report the synthesis of suspected active
Chemical process for halogenating 2-methyl-6-methoxynaphthalene
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, (2008/06/13)
A process for the preparation of a compound of formula (I): STR1 in which X and Y are identical and represent halogen, or X is halogen and Y is hydrogen, which comprises halogenating 2-methyl-6-methoxynaphthalene, of formula (II): STR2 in the presence of a free radical initiator.
Synthesis of Naphthoquinolizidines - Analogs of Cryptopleurine
Mukerjee, Y. N.,Gaur, S. P.,Jain, P. C.,Anand, Nitya
, p. 985 - 987 (2007/10/02)
Condensation of the appropriate bromomethylnaphthalene (I) with 2-(1,3-dioxa-2-cyclopentyl)pyridine followed by treatment with 48percent HBr affords 3-methoxynaphthoquinolizinium bromide (8), 3-methoxy-(9)-, 2-methoxy-(10)- and 2,3-dimethoxy-(11)-naphthoquinolizinium bromides.The compounds (8-11) on catalytic hydrogenation over PtO2 give the corresponding naphthoquinolizidines (12-15).None of these compounds show any significant anticancer activity.
