- Tetrahydrocoptisine derivative and applications thereof
-
The present invention relates to a compound as shown in a formula (VII), a preparation method and applications thereof in medicines. In particular, the present invention relates to a derivative of the compound as shown in the formula (VII), a preparation method, and the applications of the derivative used as a therapeutic agent in prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, II-type diabetes, hyperglycemia, obesity or insulin resistance syndrome and metabolic syndrome. The compound disclosed by the present invention can also reduce total cholesterol, LDL-cholesterol and triglyceride, and increases expression of a liver LDL receptor and decreases expression of PCSK9.
- -
-
-
- HIV INTEGRASE INHIBITORY OXOISOINDOLINE SULFONAMIDES
-
Novel oxoisoindoline sulfonamide integrase inhibitors are useful to inhibit HIV activity, and are therefore suitable for treatment or prophylaxis of HIV infection, for example in the treatment or prevention of AIDS. In particular embodiments, the inhibito
- -
-
Page/Page column 53
(2013/03/26)
-
- Total syntheses of HMP-Y1, hibarimicinone, and HMP-P1
-
Total syntheses of HMP-Y1, atrop-HMP-Y1, hibarimicinone, atrop-hibarimicinone, and HMP-P1 are described using a two-directional synthesis strategy. A novel benzyl fluoride Michael-Claisen reaction sequence was developed to construct the complete carbon sk
- Liau, Brian B.,Milgram, Benjamin C.,Shair, Matthew D.
-
supporting information
p. 16765 - 16772
(2013/01/15)
-
- 6,7-Dihydroxy-1-oxoisoindoline-4-sulfonamide-containing HIV-1 integrase inhibitors
-
Although an extensive body of scientific and patent literature exists describing the development of HIV-1 integrase (IN) inhibitors, Merck's raltegravir and Gilead's elvitegravir remain the only IN inhibitors FDA-approved for the treatment of AIDS. The em
- Zhao, Xue Zhi,Maddali, Kasthuraiah,Smith, Steven J.,Métifiot, Mathieu,Johnson, Barry C.,Marchand, Christophe,Hughes, Stephen H.,Pommier, Yves,Burke Jr., Terrence R.
-
supporting information
p. 7309 - 7313
(2013/02/21)
-
- Regioselective reactions of highly substituted arynes
-
"Chemical Equation Presented" The fully regioselective reactivity of four new highly substituted silyl aryl triflate aryne precursors in aryne acyl-alkylation, acyl-alkylation/ condensation, and heteroannulation reactions is reported. The application of these more complex arynes provides access to diverse natural product scaffolds and obviates late-stage functlonallzation of aromatic rings.
- Tadross, Pamela M.,Gilmore, Christopher D.,Bugga, Pradeep,Virgil, Scott C.,Stoltz, Brian M.
-
supporting information; experimental part
p. 1224 - 1227
(2010/06/13)
-
- A concise route to 3-hydroxy-4-methoxy-5-methylbenzaldehyde derivative
-
3-Hydroxy-4-methoxy-5-methylbenzaldehyde derivative (1c) has been synthesized in 7 steps from 2,3-dihydroxytoluene (4). An isopropyl derivative has been used to protect a phenol during this transformation. The overall yield of 1c was 37%.
- Saito, Naoki,Tachi, Masashi,Seki, Ryu-Ichi,Sugawara, Yayoi,Takeuchi, Eri,Kubo, Akinori
-
p. 2407 - 2421
(2007/10/03)
-
- Catechol O-methyltransferase. 12. Affinity Labeling the Active Site with the Oxidation Products of 5,6-Dihydroxyindole
-
5,6-Dihydroxyindole (5,6-DHI) and a series of 4- and/or 7-methylated analogues of 5,6-DHI have been synthesized and evaluated for their ability to inactivate purified liver rat catechol O-methyltransferase (COMT).The inactivation of COMT by these agents could be prevented by excluding oxygen from the incubation mixtures, indicating the necessity for their oxidation to the corresponding aminochromes.Substrate protection studies and kinetic studies suggested that the loss of enzyme activity resulted from the modification of a crucial amino acid residue at the active site of COMT through reaction with the quinoid oxidation products.The COMT inhibitory activity of the 4- and/or 7-methylazed analogues of 5,6-DHI argue against a mechanism involving a 1,4 Michael addition reaction at positions 4 or 7 on the aminochrome.Cnsidering the number of potential eletrophilic centers on the basic aminochrome structure, the site of the reaction might change depending on the aromatic substitution pattern.The preferred pathway of reaction may be determined in part by the juxtaposition of the protein nucleophile to the possible sites of attack on the electrophilic ligand but also in part on the reactivity of the electrophilic site which might change with substitution on the aromatic ring.
- Borchardt, Ronald T.,Bhatia, Pramila
-
p. 263 - 271
(2007/10/02)
-