- Total Synthesis of Two Glycosylated Stilbenes, Oxyresveratrol 2-O-β- d -Glucopyranoside and 2,3,5,4′-Tetrahydroxystilbene 2-O-β- d -Glucopyranoside
-
Glycosylated stilbenes are biologically active secondary metabolites of plants and have the potential to alleviate a broad range of human diseases. However, some of these compounds are not naturally abundant, and thus the synthesis of such molecules is de
- Kumar, Sunil,Lee, Hsueh-Yun,Liou, Jing-Ping
-
p. 1294 - 1301
(2017/05/31)
-
- Tyrosinase inhibitor
-
PROBLEM TO BE SOLVED: To provide a new resorcinol derivative, and further, to provide a new tyrosinase activity inhibitor composed of the resorcinol derivative. SOLUTION: There are provided the resorcinol derivative, represented by formula 1, and th
- -
-
-
- IRE-1α INHIBITORS
-
PROBLEM TO BE SOLVED: To provide compounds which directly inhibit inositol requiring enzyme 1 (IRE-1α activity) in vitro, prodrugs, and pharmaceutically acceptable salts thereof. SOLUTION: The present invention provides a compound represented by formula (A) [R3 and R4 are H or the like; Q5-Q8, together with the benzene ring to which they are attached, form a benzofused ring, where at least one of Q5-Q8 is a heteroatom selected from N, O, and S. COPYRIGHT: (C)2016,JPOandINPIT
- -
-
-
- A formal synthesis of valiolamine from myo-inositol
-
An efficient formal synthesis of racemic valiolamine starting from readily available myo-inositol is reported. In all the synthetic steps only one regioisomer is formed, which circumvents laborious purification of products. Regioselective benzylation of myo-inositol orthoformate, super-hydride mediated deoxygenation of a cyclitol derivative and stereoselective addition of dichloromethyllithium to an inosose are the key reactions in the synthesis.
- Jagdhane, Rajendra C.,Shashidhar, Mysore S.
-
p. 7963 - 7970
(2011/11/14)
-
- The stereoselective syntheses of 1-aryl-1,6-dideoxyinositol derivatives
-
This Letter describes the first report of a highly stereoselective synthesis of triethereal cyclohexanones via copper(I) mediated 1,4-addition of organometallic reagents to glucose-derived triethereal cyclohexenone. The cyclohexanones generated can be red
- Bian, Jianwei,Schneider, Steven R.,Maguire, Robert J.
-
scheme or table
p. 5417 - 5420
(2011/11/01)
-
- A new structural class of S-adenosylhomocysteine hydrolase inhibitors
-
Effective inhibitors of S-adenosylhomocysteine hydrolase hold promise towards becoming useful therapeutic agents. Since most efforts have focused on the development of nucleoside analog inhibitors, issues regarding bioavailability and selectivity have bee
- Kim, Byung Gyu,Chun, Tae Gyu,Lee, Hee-Yoon,Snapper, Marc L.
-
supporting information; experimental part
p. 6707 - 6714
(2009/12/06)
-
- Transformation of glucose into a novel carbasugar amino acid dipeptide isostere
-
The synthesis of a novel carbasugar amino acid (15), starting from D-glucose and using the Ferrier rearrangement as a key step, is reported. Compound 15 is implemented as dipeptide isostere in the synthesis of a Leu-enkephalin analog. Copyright Taylor & F
- Lastdrager, Bas,Timmer, Mattie S. M.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.,Overhand, Mark
-
-
- Biological activities of α-mangostin derivatives against acidic sphingomyelinase
-
Deprenyl and benzofenone-type congeners of α-mangostin 1 have been synthesized to understand their role for the inhibitory activity against sphingomyelinase (SMase). While removal of the prenyl group of the right side (11 and 12) caused loss of the selectivity between ASMase (acidic sphingomyelinase) and NSMase (neutral sphingomyelinase), the prenyl group of the left side appeared to increase the inhibitory activities (16 and 17).
- Hamada, Motoko,Iikubo, Kazuhiko,Ishikawa, Yuichi,Ikeda, Aya,Umezawa, Kazuo,Nishiyama, Shigeru
-
p. 3151 - 3153
(2007/10/03)
-
- The first direct synthesis of α-mangostin, a potent inhibitor of the acidic sphingomyelinase
-
A total synthesis of α-mangostin 1a has been achieved. The key cyclization reaction to construct the xanthone framework was undertaken by employing the PPh3-CCl4 conditions. The inhibitory activities of 1a and the benzophenone intermediate 16 against the acidic sphingomyelinase were discussed.
- Iikubo, Kazuhiko,Ishikawa, Yuichi,Ando, Noritaka,Umezawa, Kazuo,Nishiyama, Shigeru
-
p. 291 - 293
(2007/10/03)
-
- Substituted phenyl compounds
-
Compounds of formula (I) are described wherein R1is hydrogen, -(lower alkyl)q(CO2R6or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4and R5are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
- -
-
-
- Polyphenolic glycosides from african proteaceae
-
The phytochemical investigation of members of the genus Protea afforded a series of polyphenolic compounds (1-5) that were identified by 1D and 2D NMR experiments. Of these, 2-5 are new compounds. Chemical syntheses of 1-3 were performed in order to confirm the structures and to prepare additional material for biological evaluation.
- Verotta,Orsini,Pelizzoni,Torri,Rogers
-
p. 1526 - 1531
(2007/10/03)
-
- Selective endothelin A receptor ligands. 1. Discovery and structure-activity of 2,4-disubstituted benzoic acid derivatives
-
This paper describes the discovery of a new non-peptide endothelin A (ET(A)) selective ligand, 2,4-dibenzyloxybenzoic acid 3, which inhibits the binding of [125I]ET-1 to ET(A) receptors with an IC50 of 9 μM (ET-1 = endothelin-1). Optimisation of 3 resulted in compound 52 which had an IC50 of 1 μM. One of the analogues of 3, compound 15, was examined in a functional assay and shown to antagonise ET-1-induced contraction of rat aorta. The identification of 3 was made through the application of ChemDBS-3D searching of our corporate database. The 3D query, using an aromatic ring to a carboxylic acid group separated by 10.2 ± 1.1 A, was derived from an examination of common pharmacophoric distances found in the low energy conformations of two known ET(A) antagonists, the cyclic pentapeptide BQ 123 1 and myriceron caffeoyl ester 2.
- Astles,Brown,Handscombe,Harper,Harris,Lewis,Lockey,McCarthy,McLay,Porter,Roach,Smith,Walsh
-
p. 409 - 423
(2007/10/03)
-
- Phenolic Constituents of Glycyrrhiza Species. Part 10. Glyasperin E, a New 3-Phenoxychromen-4-one Derivative from the Roots pf Glycyrrhiza aspera
-
Glyasperin E 1, a new 3-phenoxychromen-4-one derivative, has been isolated from the roots of Glycyrrhiza aspera.The structure of glyasperin E 1 was established first on the basis of spectroscopic evidence and then confirmed by synthesis.Glyasperin E dimet
- Zeng, Lu,Fukai, Toshio,Nomura, Taro,Zhang, Ru-Yi,Lou, Zhi-Cen
-
p. 1153 - 1160
(2007/10/02)
-
- α-Glucosidase Inhibitors, 5.- Investigations towards a Synthesis of C1-Branched Cyclitols from D-Glucose
-
The glucose derivatives 1 and 2 were transformed by Ferrier rearrangement as one of the reaction steps into the cyclitol derivatives 3a,b and 4a,b, respectively.The attachment of a functional C1-side chain at the carbonyl group was tested with
- Koehn, Arnim,Schmidt, Richard R.
-
p. 1045 - 1054
(2007/10/02)
-