- NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
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Paragraph 0069; 0087
(2021/11/04)
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- Liquid crystal phosphorescent material based on cyclometalated complex and application thereof
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The invention discloses a cyclometalated organic liquid crystal phosphorescent material based on 2-phenylpyridine as a main ligand and acetylacetone as an auxiliary ligand. A benzoic acid derivative liquid crystal unit is introduced into the main ligand 2
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Paragraph 0019-0020; 0033-0034
(2021/06/09)
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- Phenoxazine-based supramolecular tetrahedron as biomimetic lectin for glucosamine recognition
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The design and synthesis of a phenoxazine-based metal-organic tetrahedron (Zn4L4) as biomimetic lectin for selectively recognition of glucosamine (GlcN) was reported. Different from the free phenoxazine-based ligand (L), Zn4L4 displayed the highest fluorescent intensity enhancement efficiency toward GlcN over other related natural mono- and disaccharides. Fluorescence titration demonstrated a 1:1 stoichiometric host-guest complex was formed with an association constant about 4.03 × 104 L/mol. 1H NMR spectroscopic studies confirmed this selectivity resulted from the multiple hydrogen bonding interactions formed between GlcN and Zn4L4. The present results suggested that rational arrangement of recognition sites in the confined space of metal-organic cage is crucial for the selectivity toward target guests.
- Li, Yuchao,Li, Xuezhao,Li, Lili,Xiao, Bing,Wu, Jinguo,Li, Hechuan,Li, Danyang,He, Cheng
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supporting information
p. 735 - 739
(2020/07/30)
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- Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
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Paragraph 0325; 0327; 0328; 0415; 0417-0419
(2020/08/28)
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- Unified Protocol for Fe-Based Catalyzed Biaryl Cross-Couplings between Various Aryl Electrophiles and Aryl Grignard Reagents
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The combination of commonly used FeCl3/SIPr with Ti(OEt)4/PhOM enabled a highly general iron-based catalyst system, which could efficiently catalyze the biaryl coupling reaction between various electrophiles (I, Br, Cl, OTs, OCONMe2, OSO2NMe2) and common or functionalized aryl Grignard reagents with high functional group tolerance. Selective couplings of aryl iodides and bromides over the corresponding oxygen-based electrophiles have been achieved, and thus a terphenyl acid intermediate for anidulafungin was conveniently synthesized via an orthogonal coupling strategy.
- Wang, Lei,Wei, Yi-Ming,Zhao, Yan,Duan, Xin-Fang
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p. 5176 - 5186
(2019/05/10)
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- Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives
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A new series of theophylline analogues containing 1,2,3-triazoles with different amide groups (22-41) has been designed and synthesized, and their biological activities have been evaluated as potential anticancer agents. The anticancer activities of the synthesized compounds were studied in four cancer cell lines viz. lung (A549), colon (HT-29), breast (MCF-7) and melanoma (A375). Furthermore, these compounds were screened for computational ADME and Lipinski's analysis followed by molecular docking and binding energy calculations against the various therapeutic targets involved in cell proliferation. The in vitro results demonstrate that compounds 22, 27, 36 and 40 have pivotal anticancer activity. Among these, compounds 22 and 27 have significant cytotoxic activity in all three cell lines; the in silico docking studies also reveal that compounds 22, 27 and 36 have good dock scores, binding affinities and binding energies towards human epidermal growth factor receptor 2. This is the first report to demonstrate theophylline hybrids containing 1,2,3-triazoles as potential anticancer agents.
- Ruddarraju, Radhakrishnam Raju,Murugulla, Adharvana Chari,Kotla, Ravindar,Tirumalasetty, Muni Chandra Babu,Wudayagiri, Rajendra,Donthabakthuni, Shobha,Maroju, Ravichandar
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supporting information
p. 176 - 183
(2017/02/05)
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- Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs
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Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).
- Beinat, Corinne,Reekie, Tristan,Banister, Samuel D.,O'Brien-Brown, James,Xie, Teresa,Olson, Thao T.,Xiao, Yingxian,Harvey, Andrew,O'Connor, Susan,Coles, Carolyn,Grishin, Anton,Kolesik, Peter,Tsanaktsidis, John,Kassiou, Michael
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supporting information
p. 277 - 301
(2015/03/31)
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- Synthesis of new bioorganometallic Ir- and Rh-complexes having β-lactam containing ligands
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The synthesis (and full spectroscopic and crystallographic characterization) of new classes of bioorganometallic Ir- and Rh-complexes having β-lactam containing ligands has been achieved in three steps starting from simple precursors. The procedure for preparing these bioorganometallic compounds uses β-lactams having a phenylpyridyl moiety attached to the C4, N1 or C4 and N1 positions simultaneously, and a directed C-H metal-insertion, in the presence of (MCp*Cl2)2 (M = Ir, Rh). Enantiomerically pure 2-azetidinones can be transformed into diastereomeric (at the metal) mixtures of enantiopure metalla-2-azetidinones. Bimetallic 2-azetidinones are also accessible by this approach. The insertion of electron-poor alkynes into the M-C bond of the bioorganometallic complex occurs regioselectively and in excellent yields. Overall, the sequence imine-β-lactam-metalla-β-lactam is a versatile and efficient full methodology to prepare and functionalize unprecedented, novel Ir- and Rh-complexes having β-lactam containing ligands.
- Muntaner, Jaime G.,Casarrubios, Luis,Sierra, Miguel A.
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supporting information
p. 286 - 297
(2014/01/06)
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- COMPOUND HAVING NPY Y5 RECEPTOR ANTAGONIST ACTIVITY
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This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.
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Page/Page column 32
(2011/02/25)
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- COMPOUNDS HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY
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This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.
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Page/Page column 20
(2011/02/25)
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- 2-Pyridyl and 3-pyridylzinc bromides: direct preparation and coupling reaction
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A facile synthetic approach to the direct preparation of 2-pyridyl and 3-pyridylzinc bromides has been demonstrated using Rieke zinc with 2-bromopyridine and 3-bromopyridine, respectively. A variety of different electrophiles have been coupled with the resulting organozinc reagents to give the corresponding cross-coupling products in moderate to good yields.
- Kim, Seung-Hoi,Rieke, Reuben D.
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scheme or table
p. 3135 - 3146
(2010/06/13)
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- Coupling reactions with haloaromatic amines and alcohols for a practical synthetic route to 2-substituted aminophenyl and hydroxyphenyl pyridines
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A practical synthetic route to 2-substituted aminophenyl and hydroxyphenyl pyridines has been developed. It has been accomplished by the cross-coupling reactions of readily available 2-pyridylzinc bromides with haloaromatic amines and alcohols under mild
- Kim, Seung-Hoi,Rieke, Reuben D.
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supporting information; experimental part
p. 6985 - 6988
(2010/02/27)
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- Synthesis of functionalized 2-arylpyridines from 2-halopyridines and various aryl halides via a nickel catalysis
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An efficient nickel-catalyzed method devoted to the direct formation of functionalized 2-arylpyridines is described avoiding the prior preparation of organometallic species. Various functionalized 2-arylpyridines are obtained in moderate to excellent yields by a one-step chemical procedure from corresponding halides. The NiBr2(2,2′-bipyridine) complex appears to be an extremely suitable catalyst for the activation in the presence of manganese dust of aromatic halides and pyridyl halides functionalized by reactive groups. The versatility of this original process represents a simple alternative to most known methods using organometallic reagents.
- Gosmini, Corinne,Bassene-Ernst, Carine,Durandetti, Muriel
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experimental part
p. 6141 - 6146
(2011/03/19)
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- CAPREOMYCIN DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
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The present invention relates to phenylurea derivatives of capreomycin I, IIB, IIA, or IB, and metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are useful as antibacterial agents for treating b
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Page/Page column 63
(2008/06/13)
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- Capreomycin derivatives and their use as antibacterials
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The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial
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Page/Page column 22
(2008/06/13)
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- TETRAHYDROISOQUINOLINES AS FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 33
(2008/06/13)
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- Orally active CCR5 antagonists as anti-HIV-1 agents 2: Synthesis and biological activities of anilide derivatives containing a pyridine N-oxide moiety
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In order to develop orally active CCR5 antagonists, we investigated 1-benzoxepine derivatives containing new polar substituents, such as phosphonate, phosphine oxide or pyridine N-oxide moieties, as replacements for the previoiusly reported quaternary ammonium moiety. Among these compounds, the 2-(α-hydroxybenzyl)pyridine N-oxide 5e exhibited moderate CCR5 antagonistic activity and had an acceptable pharmacokinetic profile in rats. Subsequent chemical modification was performed and compound (S)-5f possessing the (S)-configuration hydroxy group was found to be more active than the (R)-isomer. Replacement of the 1-benzoxepine ring with a 4-methylphenyl group by a 1-benzazepine ring with a 4-[2-(butoxy)ethoxy]phenyl group enhanced the activity in the binding assay. In addition, introduction of a 3-trifluoromethyl group on the phenyl group of the anilide moiety led to greatly increased activity in the HIV-1 envelope-mediated membrane fusion assay. In particular, compound (S)-5s showed the most potent CCR5 antagonistic activity (IC 50=7.2 nM) and inhibitory effect (IC50=5.4 nM) in the fusion assay, together with good pharmacokinetic properties in rats.
- Seto, Masaki,Aramaki, Yoshio,Imoto, Hiroshi,Aikawa, Katsuji,Oda, Tsuneo,Kanzaki, Naoyuki,Iizawa, Yuji,Baba, Masanori,Shiraishi, Mitsuru
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p. 818 - 829
(2007/10/03)
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- The preparation of a stable 2-pyridylboronate and its reactivity in the Suzuki-Miyaura cross-coupling reaction
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The preparation and reactivity of a 2-pyridylboronate stabilised by N-phenyldiethanolamine is described. In Suzuki-Miyaura cross-coupling reactions employing this boronate, significant aryl-aryl exchange from the phosphine ligand was observed with some combinations of ligand and substrates. The amount of the exchange by-product can be minimised by appropriate choice of phosphine ligand.
- Hodgson, Paul B.,Salingue, Fabrice H.
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p. 685 - 687
(2007/10/03)
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- Electrochemical cross-coupling between 2-halopyridines and aryl or heteroaryl halides catalysed by nickel-2,2'-bipyridine complexes
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2-Arylpyridines can be obtained in good to high yields by electrochemical reductin using the sacrificial anode process and catalysis by nickel-2,2'-bipyridine (bpy) complexes. In a first approach functionalized arylzinc species are prepared in DMF as solvent by electrolytic reduction of the corresponding aryl-bromides or -chlorides in the presence of ZnBr2 and Ni(II)-bpy complexes and then coupled with 2-chloropyridine. In a second approach the cross-coupling occurs from the electrochemical reduction of a stoichiometric mixture of an aryl halide and 2-halopyridine in DMF in the presence of NiBr2bpy as catalyst.
- Gosmini, Corinne,Lasry, Sarah,Nedelec, Jean-Yves,Perichon, Jacques
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p. 1289 - 1298
(2007/10/03)
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- INDOLE DERIVATIVES. 133. SYNTHESIS OF 5-(2-PYRIDYL)INDOLE
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Starting from 2-(4-nitrophenyl)pyridine, the product of the Gomberg arylation of pyridine, 5-(2-pyridyl)indole was prepared by the Japp-Klingman reaction. 13C NMR indicated an inductively transmitted interaction between the pyridine and indole rings.
- Akhvlediani, R. N.,Khazhidze, M. M.,Eraksina, V. N.,Suvorov, N. N.
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p. 1221 - 1225
(2007/10/02)
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- PROPERTIES OF THE LIQUID CRYSTALS FORMED BY CERTAIN 4-(2 prime -PYRIDYL)PHENYL AND 4-(4 prime -PYRIDYL)PHENYL 4 double prime -N-ALKOXYBENZOATES.
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Nine members of each of two homologous series of esters, the 4-(2 prime -pyridyl)phenyl and the 4-(4 prime -pyridyl)phenyl 4 double prime -n-alkoxybenzoates, were prepared and their liquid crystal transition temperatures measured. Both homologous series w
- Byron,Lacey,Wilson
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p. 103 - 114
(2007/10/02)
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