Synthetic Utility Of Glycopeptide Glycosyltransferases

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A Systematic Investigation of the Synthetic Utility of Glycopeptide Glycosyltransferases. - Oberth ü r et al. J. Am. Chem. Soc. 2005 , 127 , 10747-10752.

Glycosylated natural products Biochemical Society Transactions 2003, 31(3), 487

Manipulation of D-glucose to give L-epi-vancosamine PNAS 2000, 97 (22), 11942.

Glycosylation pathway for the maturation of chloroeremomycin. PNAS 2004 101(13), 4390

Synthetic strategy toward TDP  -2-deoxy sugars 3 - 6 and 9 TDP sugars used for the study of specificity of GtfA, C and D Org. Lett., 2004, 6 (17), 2873.

Glycosylation of vancomycin pseudoaglycon 1 with Gtf A, C and D

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The ambiguity of whether aldose reductase, an enzyme of polyol pathway, is linked to diabetes and its complication has been receded based on the recent studies made on the inhibition of its (Aldose reductase) activity. In our current study, we have used an in silico approach (molecular docking) to analyze the effect of essential phytochemicals obtained from Cymbopogon citratus on the aldose reductase activity. C.citratus is grown extensively in tropical countries including India for perfumery and pharmaceuticals. The essential phytochemicals of C.citratus like Myrcene, Citral, and Geraniol have been used as ligand for the molecular docking analysis with Aldose reductase as receptor. The docking analysis showed Myrcene, with binding energy of -8.76 Kcal/mol is best amongst Citral and Geraniol which are having binding energies of -7.24 Kcal/mol and -7.93 Kcal/mol respectively for inhibiting the activity of Aldose reductase.

Inhibition of Aldose Activity by Essential Phytochemicals of Cymbopogon citra...

CSCJournals

medicine due to their significant role in the treatment of different health problems. Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the Claisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d). In vitro cytotoxic activity of the synthesized compounds was studied against four different selected human cancer cell lines by using sulforhodamine B (SRB) method. Results: The adopted scheme resulted in good yields of new series of isoxazole-chalcone conjugates (14a-m). Potent cytotoxic activity was observed for compounds -14a, 14b, 14e, 14i, 14j and 14k against prostate DU-145 cancer cell line. Conclusion: The observed potent cytotoxic activities were due to the presence of 3,4,5- trimethoxyphenyl group.

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:We developed the novel polymeric prodrugs synthesized by mechanochemical solid-state copolymerization of glucose-based polysaccharides (dextran orglycogen) and the methacryloyloxy derivative of 5-fluorouracil (5-FU). The copolymerization proceededreadily and each polymeric prodrug was quantitatively obtained within8 h reaction. The number average molecular weight (Mn) and polydispersity (H) of the polymeric prodrug synthesized from dextran was 24,000 g/mol and 5.10, respectively. The number average particle diameter of the polymeric prodrug derived from glycogen was 14.9 nm. The hydrolysis profiles of the polymeric prodrug synthesized from dextranapparently followed the first-order kinetics, and 100% drug release was observed under the experimental condition used. The polymeric prodrug derived from glycogen also continued to release 5-FU at the first-order rate up to 5 h, followed by its rate constant decreased gradually. These results suggest that lower accessibility of water molecules for the synthetic polymer chains inside the glycogen particle might cause the gradual decrease of drug release rate.

A Novel Polymeric Prodrugs Synthesized by Mechanochemical Solid-State Copolym...

inventionjournals

The study aims at the comparative study of once-daily ziprasidone loaded polymeric microspheres-based (ZEmsp) matrix tablets (ZEmsp-T) as a sustained delivery system with conventional matrix tablets. The effect of variation in the drug/polymer ratio on the physicochemical characteristics of the microspheres was investigated. The optimized ZEmsp formulation demonstrated favorable mean particle size and drug loading along with sustained release pattern. After the selection of the optimized microspheres, matrix tablets were compressed with different direct tableting agents. After successful preparation and evaluation of ZEmsp-T, we found that batch ZEmsp-T3 and ZEmsp-T4, respectively. The optimized matrix tablets showed sustained release pattern of the drug release. The same parameters were evaluated for conventional matrix tablets, but results were not complies. Thus, results of this study prove the suitability of using Eudragit RSPO as a sustained release polymeric material to develop microspheres combined with different tableting agents to prepared matrix tablets were designed successfully for once-daily oral administration to avoid dosing frequency

Comparison between Oral Delivery of Eudragit RSPO Microsphere-Based Matrix Ta...

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Design and Synthesis of a Novel Thiolate Histone Deacetylase Inhibitor

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Springer

Total synthesis of natural products

Springer

Alzheimers - Tideglusib presentation

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Crocin, the main constituent of Crocus sativus L., protected against infl ammation-induced neurotoxicity and improved learning behavior. Also, crocin inhibited production of inducible nitric oxide synthase. Studies also indicated an interaction between NO and Formaldehyde (FA) -induced neurotoxicity. In this study, effect of crocin on memory and body weight changes in neurotoxicity induced by FA was evaluated in a rat model. Moreover, the possible involvement of NO on protective effects of crocin was investigated. FA (5 mg/kg) was administered intraperitoneally for 5 consecutive days. Effect of crocin post-treatment (25, 50 and 100 mg/kg, i.p.) on FA neurotoxicity was evaluated on passive avoidance memory.

Advanced Journal of Toxicology: Current Research

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Synthesis, characterization, amdet and docking studies of novel diclofenac de...

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Inhibition of Aldose Activity by Essential Phytochemicals of Cymbopogon citra...

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Total synthesis of natural products

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