- PYRIDINE COMPOUND SUBSTITUTED WITH AZOLE
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The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R1, R2, R3, and R4 independently represent a hydrogen atom, a fluorine atom, methyl, or the like, R5 represents any of the structures represented by formula group [IV]:
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Paragraph 0940
(2020/07/07)
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- Metal-Free Tandem Rearrangement/Lactonization: Access to 3,3-Disubstituted Benzofuran-2-(3H)-ones
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A novel metal-free synthesis of 3,3-disubstituted benzofuran-2-(3H)-ones through reacting α-aryl-α-diazoacetates with triarylboranes is presented. Initially, triarylboranes were successfully investigated in α-arylations of α-diazoacetates, however in the presence of a heteroatom in the ortho position, the boron enolate intermediate undergoes an intramolecular rearrangement to form a quaternary center. The intermediate cyclizes to afford valuable 3,3-disubstituted benzofuranones in good yields.
- Santi, Micol,Ould, Darren M. C.,Wenz, Jan,Soltani, Yashar,Melen, Rebecca L.,Wirth, Thomas
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supporting information
p. 7861 - 7865
(2019/04/25)
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- (2-Benzyloxyphenyl)acetyl (BnPAc): A Participating Relay Protecting Group for Diastereoselective Glycosylation and the Synthesis of 1,2-trans Glycosyl Esters
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The (2-benzyloxyphenyl)acetyl group has been identified as a new protecting group for hydroxyl functions. Various alcohols could be easily protected with high yields, and deprotection was achieved by a relay approach using Pd/H 2 in combination with 1,8-bis(dimethylamino)naphthalene, conditions that are orthogonal to ester groups. The new protecting group is stable in glycosylation reactions demonstrating an effective neighboring group participation leading to the exclusive formation of 1,2-trans glycosides and glycosyl esters.
- Weber, Julia,Krauter, Simon,Schwarz, Theresa,Hametner, Christian,Mikula, Hannes
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p. 2265 - 2268
(2018/10/20)
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- Total synthesis and stereochemical revision of xiamenmycin A
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The relative and absolute configurations of xiamenmycin A, a benzopyran compound isolated from Streptomyces xiamenensis 318 with a highly potent anti-fibrotic activity, have been characterized through the total synthesis. The key steps include the constru
- Jiao, Xiaozhen,Yao, Yangyang,Yang, Beibei,Liu, Xiaoyu,Li, Xiaoyu,Yang, Hongguang,Li, Li,Xu, Jun,Xu, Minjuan,Xie, Ping
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p. 1805 - 1813
(2016/02/10)
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- Synthesis and in vitro antitumor activity of asperphenamate derivatives as autophagy inducer
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In an effort to improve the aqueous solubility and the antitumor activity of natural product asperphenamate, we have designed and synthesized three series of asperphenamate derivatives, including series I (simplifying molecular skeleton series), series II (introducing a hydroxyl group to A-phenyl ring series) and series III (disrupting molecular planarity series). All derivatives have displayed a significantly increased solubility compared with asperphenamate. Their growth inhibitory activities in vitro were screened by the standard MTT method in MCF-7, HeLa, and BEL-7402 cell lines. With the exception of the derivatives in series I, most of derivatives in series II and series III showed growth inhibitory activity. Among all derivatives, IM23b in series III showed the greatest potency in human breast cancer MCF-7 cells. The cellular potency of IM23b was approximately 1.5-fold more potent than that of cisplatin. The mechanism of cell death induced by IM23b in human breast cancer MCF-7 cells was further investigated. We concluded that the cell death was induced by autophagy instead of apoptosis or cell cycle arrest.
- Yuan, Lei,Li, Yanchun,Zou, Chunyang,Wang, Chao,Gao, Jian,Miao, Caixia,Ma, Enlong,Sun, Tiemin
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scheme or table
p. 2216 - 2220
(2012/04/18)
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- Substituted compounds derived from N-(benzyl)phenylacetamide, preparation and uses
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This invention relates to poly-substituted derivatives of the N-(benzyl)phenylacetamide type, pharmaceutical compositions comprising same, therapeutic uses thereof, more particularly in the fields of human and animal health. This invention also relates to a process for the preparation of such derivatives.
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Page/Page column 50
(2010/10/20)
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- 2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands
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A series of 2-benzyl and 2-phenyl-3-hydroxypropyl pivalates designed to incorporate the principal pharmacophores of phorbol esters have been synthesized and tested as PKC-α ligands. Among the analogues, 13c exhibited the most potent binding affinity with a Ki = 0.7 μM. The synthesized analogues were subjected to molecular modeling analysis based on two alternative models of the phorbol pharmacophore and a docking study of 13c was carried out.
- Lee, Jeewoo,Lee, Ju-Hyun,Kim, Su Yeon,Perry, Nicholas A.,Lewin, Nancy E.,Ayres, Jolene A.,Blumberg, Peter M.
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p. 2022 - 2031
(2007/10/03)
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- Endothelin antagonists
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A compound of formula (I), in which: R1is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R2is hydrogen, hydroxy or protected h
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- Efficient synthesis of 1-Benzyloxyphenyl-3-phenylacetones
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1-[(Benzyloxy)phenyl]-3-phenylacetones 1a-c have been conveniently synthesized by acylation of the PhCH2Li-DABCO complex with their respective N-methyl O-methyl hydroxamates 5a-c. In four steps, ketones 1a-c having ortho-, meta- and para-benzyloxy substituents were obtained in 42-51% overall yields from commercially available 2-(hydroxyphenyl)acetic acids.
- Mannekens,Tourwe,Lubell
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p. 1214 - 1216
(2007/10/03)
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- Polymer-Supported Mitsunobu Ether Formation and its Use in Combinatorial Chemistry
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Aromatic hydroxy acids have been attached to a polymeric solid support and the phenolic hydroxy groups have been reacted with a variety of primary and secondary alcohols under the conditions of the Mitsunobu reaction (triphenylphosphine and diethyl azodicarboxylate) in tetrahydrofuran.In most cases the reaction provided a nearly quantitative yield of alkyl aryl ethers, as determined after cleaving theproduct from the resin.To demonstrate that the polymer-supported Mitsunobu reaction is useful for combinatorial library synthesis, we synthesized a number of model compounds and a simple three randomization step library composed of 4,200 different compounds.
- Krchnak, Viktor,Flegelova, Zuzka,Weichsel, Aleksandra S.,Lebl, Michal
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p. 6193 - 6196
(2007/10/02)
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- SYNTHETIC METHODS. PART 23. REARRANGEMENT OF SOME HYDROXAMIC ACIDS INTO AMIDES. A SELF-CONDENSATION LEADING TO DISPROPORTIONATION
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Pyruvic acids have been shown to react with p-nitroso-N,N-dimethylaniline (1) to produce p-dimethyl-aminoacetanilides (3) via the corresponding hydroxamic acids (4).Three such intermediates (4a, c, d) have been isolated and their structure proved by n.m.r. and mass spectroscopy and elemental analysis.Solutions of the hydroxamic acids (4) have been shown to undergo concentration-dependent self-condensation and disproportionation leading to the amides (3) and acids (5).Rational pathways for these transformations are discussed.Spectral correlations permit differentiation between the amides (3) and the corresponding hydroxamic acids (4).
- Hassner, Alfred,Ruse, Margareta,Gottlieb, Hugo E.,Cojocaru, Miriam
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p. 733 - 738
(2007/10/02)
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