- New glucocerebrosidase inhibitors by exploration of chemical diversity of N -substituted aminocyclitols using click chemistry and in situ screening
-
A library of aminocyclitols derived from CuAAC reaction between N-propargylaminocyclitol 4 and a series of azides [1′25] is described and tested against GCase. Azides have been chosen from a large collection of potential candidates that has been filtered
- Díaz, Lucía,Casas, Josefina,Bujons, Jordi,Llebaria, Amadeu,Delgado, Antonio
-
supporting information; experimental part
p. 2069 - 2079
(2011/06/10)
-
- Dendrimer analogues of linear molecules to evaluate energy and charge-transfer properties
-
We have designed and synthesized difunctionalized dendrimers containing two donors in the periphery and an acceptor at the core to serve as scaffolds for comparison with linear analogues to investigate the advantage of dendritic scaffolds for energy and c
- Nantalaksakul, Arpornrat,Dasari, Raghunath Reddy,Ahn, Tai-Sang,Al-Kaysi, Rabih,Bardeen, Christopher J.,Thayumanavan
-
p. 2981 - 2984
(2007/10/03)
-
- The first total synthesis of SB87-Cl and pestalone, novel bioactive benzophenone natural products
-
SB87-Cl 1, an inhibitor of testosterone-5α-reductase, and pestalone 2 exhibiting effective antimicrobial activity against MRSA (MIC=37ng/mL) and VRE (MIC=78ng/mL), were novel bioactive benzophenone natural products. Total synthesis of 1 and 2 has been successfully accomplished. The common synthetic precursor 18 of 1 and 2, was successfully obtained by the coupling of 8 with 12.
- Iijima, Daisuke,Tanaka, Daisuke,Hamada, Motoko,Ogamino, Takahisa,Ishikawa, Yuichi,Nishiyama, Shigeru
-
p. 5469 - 5471
(2007/10/03)
-
- 5-MEMBERED N-HETEROCYCLIC COMPOUNDS WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY
-
Use of a compound of the formula: wherein R represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; X represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: -CO-, -CS-, -CR(OR)- or -NR- wherein each of R and R represents a hydrogen atom or a hydrocarbon group which may be substituted, R represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: -SO-, -SO2-, -NR-, -CONR- or -NRCO- wherein R represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group; X represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: -SO-, -SO2-, -O-SO2- or -NR- wherein R represents a hydrogen atom or a hydrocarbon group which may be substituted; R represents a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; W represents a bond or a divalent hydrocarbon residue having 1 to 20 carbon atoms; R represents a group of the formula: -OR (R represents a hydrogen atom or a hydrocarbon group which may be substituted) or -NRR (each of R and R, whether identical or not, represents a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; R and R may bind together to form a ring); or a salt thereof, for the manufacture of a pharmaceutical preparation for preventing or treating syndrome X.
- -
-
-
- Mechanistic studies on the biomimetic reduction of tetrahydroxynaphthalene, a key intermediate in melanin biosynthesis
-
1,3,6,8-Tetrahydroxynaphthalene (T4HN) is an aromatic polyketide, serving as a general precursor of fungal melanin. Melanin biosynthesis involves two consecutive deoxygenations of T4HN, consisting of the reduction of a phenolic carbon followed by dehydrat
- Ichinose,Ebizuka,Sankawa
-
p. 192 - 196
(2007/10/03)
-
- Alternative convergent and accelerated double-stage convergent approaches towards functionalized dendritic polyethers
-
Alternative convergent synthesis strategies for the preparation of dendritic macromolecules, using either mesylate activation or the Mitsunobu reaction, are described. The synthesis can be further accelerated by using a double stage convergent approach. T
- Forier,Dehaen
-
p. 9829 - 9846
(2007/10/03)
-
- DEOXYGENATION IN THE BIOSYNTHESIS OF POLYKETIDES: MECHANISM OF BIOMIMETIC REDUCTION OF TETRAHYDROXYNAPHTHALENE
-
A biomimetic synthesis of scytalone, a simple derivative of tetralone, was reinvestigeted using NMR spectroscopy.Scytalone was formed from 1,3,6,8-tetrahydroxynaphthalene (1,3,6,8-THN) by sodium borohydride reduction only in the presence of sodium methoxi
- Ichinose, Koji,Ebizuka, Yutaka,Sankawa, Ushio
-
p. 2873 - 2875
(2007/10/02)
-
- Drugs derived from Cannabinoids. Part 8. The Synthesis of Side-chain Analogues of Δ6a,10a-Tetrahydrocannabinol
-
The continuation of studies on the synthesis of side-chain analogues of Δ6a,10a-tetrahydrocannabinol as potential therapeutic agents has led to the syntheses of a possible metabolite 1-hydroxy-6,6,9-trimethyl-7,8,9,10-tetrahydro-6H-dibenzopyran-3-ylacetic acid (1) and 2-(1-hydroxy-6,6,9-trimethyl-7,8,9,10-tetrahydro-6H-dibenzopyran-3-yl)pent-4-ynoic acid (17c).The Pechmann condensation of ethyl 4-methyl-2-oxocyclohexane-1-carboxylate with methyl 3,5-dihydroxyphenylacetate (11), followed by Grignard reaction, was utilized to produce the pyran (1).The key step in the synthesis of the propargylacetic acid (17c) was propargylation of the malonate (15) under phase-transfer catalysis.
- Meltzer, Peter C.,Dalzell, Haldean C.,Razdan, Raj K.
-
p. 2825 - 2829
(2007/10/02)
-