- Different structures of the two peroxisome proliferator-activated receptor gamma (PPARγ) ligand-binding domains in homodimeric complex with partial agonist, but not full agonist
-
We designed and synthesized acylsulfonamide derivative (3) as a human peroxisome proliferator-activated receptor gamma (hPPARγ) partial agonist by structural modification of hPPARγ full agonist 1. Co-crystallization of 3 with hPPARγ LBD afforded a homodim
- Ohashi, Masao,Oyama, Takuji,Miyachi, Hiroyuki
-
-
Read Online
- Structural design and synthesis of arylalkynyl amide-type peroxisome proliferator-activated receptor γ3 (PPAR γ3)-selective antagonists based on the helix12-folding inhibition hypothesis
-
Peroxisome proliferator-activated receptor γ3 (PPARγ3) antagonists are candidates for treatment of type 2 diabetes, obesity and osteoporosis. However, few rational design strategies are currently available. Here, we utilized the helix12 (H12)-folding inhi
- Ohashi, Masao,Gamo, Kanae,Tanaka, Yuta,Waki, Minoru,Beniyama, Yoko,Matsuno, Kenji,Wada, Jun,Tenta, Masafumi,Eguchi, Jun,Makishima, Makoto,Matsuura, Nobuyasu,Oyama, Takuji,Miyachi, Hiroyuki
-
-
- Enhanced Reactivity of Aerobic Diimide Olefin Hydrogenation with Arylboronic Compounds: An Efficient One-Pot Reduction/Oxidation Protocol
-
A catalyst-free and efficient method for simultaneous olefin hydrogenation and oxidation of arylboronate esters to phenols with hydrazine hydrate and molecular oxygen is presented. The process is based on the utilization of a readily available Lewis acidic arylboron compound, which evades common problems associated with the catalyst-free aerobic hydrogenation of olefins with diimide. Using an operationally simple procedure, the protocol smoothly delivers phenol derivatives and various alkanes in excellent yields with remarkable functional group compatibility. The method allows the reaction to be scaled up to 1 g of the starting materials.
- Santra, Surojit,Guin, Joyram
-
supporting information
p. 7253 - 7257
(2015/11/25)
-
- Pd/C-catalyzed chemoselective hydrogenation in the presence of diphenylsulfide
-
A Pd/C-catalyzed chemoselective hydrogenation using diphenylsulfide as a catalyst poison has been developed. This methodology selectively hydrogenates olefin and acetylene functionalities without hydrogenolysis of aromatic carbonyls and halogens, benzyl esters, and N-Cbz protective groups.
- Mori, Akinori,Miyakawa, Yumi,Ohashi, Eri,Haga, Tomoko,Maegawa, Tomohiro,Sajiki, Hironao
-
p. 3279 - 3281
(2007/10/03)
-
- Chemoselective hydrogenation method catalyzed by Pd/C using diphenylsulfide as a reasonable catalyst poison
-
While Pd/C is one of the most useful catalysts for hydrogenation, the high catalyst activity of Pd/C causes difficulty in its application to chemoselective hydrogenation between different types of reducible functionalities. In order to achieve chemoselective hydrogenation using Pd/C, we investigated catalyst poison as a controller of the catalyst activity. We found that the addition of Ph2S (diphenylsulfide) to the Pd/C-catalyzed hydrogenation reaction mixture led to reasonable deactivation of Pd/C. By the use of the Pd/C-Ph2S catalytic system, olefins, acetylenes, and azides can be selectively reduced in the coexistence of aromatic carbonyls, aromatic halides, cyano groups, benzyl esters, and N-Cbz (benzyloxycarbonyl) protecting groups. The present method is promising as a general and practical chemoselective hydrogenation process in synthetic organic chemistry.
- Mori, Akinori,Mizusaki, Tomoteru,Miyakawa, Yumi,Ohashi, Eri,Haga, Tomoko,Maegawa, Tomohiro,Monguchi, Yasunari,Sajiki, Hironao
-
p. 11925 - 11932
(2007/10/03)
-
- Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents
-
It has been reported that 2-hydroxycinnamaldehyde and 2-benzoyl- oxycinnamaldehyde inhibited the activity of farnesyl protein transferase, angiogenesis, cell-cell adhesion, and tumor growth in vivo model. In order to improve its anti-tumor activity, dimer
- Shin, Dae-Seop,Kim, Jong-Han,Lee, Su-Kyung,Han, Dong Cho,Son, Kwang-Hee,Kim, Hwan-Mook,Cheon, Hyae-Gyeong,Kim, Kwang-Rok,Sung, Nack-Do,Lee, Seung Jae,Kang, Sung Kwon,Kwon, Byoung-Mog
-
p. 2498 - 2506
(2007/10/03)
-
- Highly chemoselective hydrogenation method using novel finely dispersed palladium catalyst on silk-fibroin: Its preparation and activity
-
A palladium-fibroin complex (Pd/Fib) was prepared by soaking silk-fibroin in MeOH solution of Pd(OAc)2 for 2 days (under Ar atmosphere) - 4 days (under air). Pd(OAc)2 was gradually absorbed by fibroin and the rapid reduction of fibroin conjugated Pd(OAc)2 proceeded with MeOH as a reductant at room temperature to be the Pd(0) complex. Pd/Fib catalyzed chemoselective hydrogenation of acetylenes, olefins and azides in the presence of aromatic ketones and aldehydes, halides, N-Cbz protective groups and benzyl esters which are readily hydrogenated using Pd/C or Pd/C(en) as a catalyst.
- Ikawa, Takashi,Sajiki, Hironao,Hirota, Kosaku
-
p. 2217 - 2231
(2007/10/03)
-
- Cinnamaldehyde derivatives inhibiting growth of tumor cell and regulating cell cycle, preparations and pharmaceutical compositions thereof
-
The present invention relates to cinnamaldehyde derivatives inhibiting growth of tumor cell and regulating cell cycle, the method for preparation and the pharmaceutical composition thereof. The cinnamaldehyde derivatives of the present invention can be ef
- -
-
-
- Preparation of silk fibroin-supported Pd(0) catalyst for chemoselective hydrogenation: Reduction of palladium(II) acetate by methanol on the protein
-
The Pd/fibroin (Fib) was easily prepared by the auto-reduction of the silk-fibroin conjugated Pd(OAc)2 using MeOH as a solvent and a reductant and exhibited good chemoselectivity in the hydrogenation of olefins and azides in the presence of aromatic carbonyls and/or halogens or an O-benzyl protective group.
- Sajiki, Hironao,Ikawa, Takashi,Yamada, Hiromi,Tsubouchi, Kozo,Hirota, Kosaku
-
p. 171 - 174
(2007/10/03)
-
- Compositions containing aromatic aldehydes and their use in treatments
-
Disclosed are pharmaceutical and cosmetic compositions containing aromatic aldehyde compounds. Some of the disclosed compositions are useful as topical therapeutics for treating inflammatory dermatologic conditions. Some of the compositions are useful in transdermal and other systemic dose forms for treating other inflammatory conditions in mammals.
- -
-
-
- Cyclic compounds and uses thereof
-
Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1is an optionally substituted five- or six-membered ring group; X1is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1and E4are each optionally substituted carbon or the like; E2and E3are each oxygen or the like; and a and b are each a single bond or a double bond); X2is a divalent group constituting a straight chain moiety; Z1is a divalent cyclic group or the like; Z2is a free valency or the like; and R2is optionally substituted amino or the like.
- -
-
-
- 6-aryl pyrazolo?3,4-D! pyrimidin-4-ones and compositions and method of use thereof
-
6-Aryl pyrazolo?3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.
- -
-
-
- Radical isomerization via intramolecular ipso substitution of aryl ethers: Aryl translocation from oxygen to carbon
-
Bromopropyl aryl ethers an converted to 3-arylpropanols under standard radical generating conditions in the presence of tributylstannane and AIBN. This rearrangement involves intramolecular ipso attack of the alkyl radicals which generates spiro cyclohexadienyl radical intermediates.
- Lee, Eun,Lee, Chulbom,Tae, Jin Sung,Whang, Ho Sung,Li, Kap Sok
-
p. 2343 - 2346
(2007/10/02)
-
- Photocyclization Reactions. Part 1. Synthesis of Dihydrobenzofuranols Using Photocyclization of 2-Alkoxybenzaldehydes, 2'-Alkoxyacetophenones, 2-Formylphenoxyacetic Acids and 2-Acetylphenoxyacetic Acids
-
Photocyclization reactions were carried out on 2-alkoxybenzaldehydes 1a-f, 2'-alkoxyacetophenones 2a-h, 2-formylphenoxyacetic acids 1i-l and 2-acetylphenoxyacetic acids 2i-m.Irradiation opf 1a-f and 2a-h in acetonitrile gave the corresponding dihydrobenzofuranols 3, 5 and dihydroisobenzofuranols 4, 6.Using carboxylic acids 1i-l, 2i-m as starting materials, decarboxylation occurred immediately to give the corresponding ethers 1a-d, 2a-e.Further irradiation of the solution afforded dihydrobenzofuranols 3,5 and dihydroisobenzofuranols 4, 6.Substituent effects on photocyclization and reaction pathways are discussed.
- Horaguchi, Takaaki,Tsukada, Chikara,Hasegawa, Eietsu,Shimizu, Takahachi,Suzuki, Tsuneo,Tanemura, Kiyoshi
-
p. 1261 - 1272
(2007/10/02)
-
