- Novel π-conjugated molecules based on diimidazopyridine: Significantly improved the photophysical, thermal and electrochemical properties bearing different aryl substituents
-
A series of π-conjugated molecules based on diimidazolepyridine derivatives were designed, synthesized by Suzuki coupling reaction and cyclization reaction and characterized. Diimidazolepyridine motif as the main structure could improve the thermal stabil
- Huang, Xin,Tian, Jinchang,Xu, Feng,Liu, Xiaochong,Li, Yuqin,Guo, Yanyan,Chu, Wenyi,Sun, Zhizhong
-
-
Read Online
- BENZIMIDAZOLE COMPOUNDS AND USE THEREOF FOR TREATING ALZHEIMER'S DISEASE OR HUNTINGTON'S DISEASE
-
Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.
- -
-
Page/Page column 13; 18; 19; 52
(2020/03/23)
-
- BENZIMIDAZOLE COMPOUNDS AND USE THEREOF FOR TREATING ALZHEIMER'S DISEASE OR HUNTINGTON'S DISEASE
-
Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.
- -
-
Paragraph 0038; 0045; 0175-0176
(2020/03/23)
-
- Discovery of novel “Dual-site” binding oseltamivir derivatives as potent influenza virus neuraminidase inhibitors
-
From our research group, it was noticed that oseltamivir derivatives targeting 150-cavity of neuraminidase enzyme (NA) could significantly increase antiviral activity. Thus, we further enriched the C5–NH2 position of oseltamivir structure to ob
- Ai, Wei,Cherukupalli, Srinivasulu,Ding, Xiao,Huang, Bing,Jia, Ruifang,Jiang, Xiangyi,Li, Zhong,Liu, Xinyong,Ma, Xiuli,Sun, Lin,Sun, Zhuosen,Wang, Defeng,Zalloum, Waleed A.,Zhan, Peng,Zhang, Jian
-
-
- Evaluation of α-hydroxycinnamic acids as pyruvate carboxylase inhibitors
-
Through a structure-based drug design project (SBDD), potent small molecule inhibitors of pyruvate carboxylase (PC) have been discovered. A series of α-keto acids (7) and α-hydroxycinnamic acids (8) were prepared and evaluated for inhibition of PC in two assays. The two most potent inhibitors were 3,3′-(1,4-phenylene)bis[2-hydroxy-2-propenoic acid] (8u) and 2-hydroxy-3-(quinoline-2-yl)propenoic acid (8v) with IC50 values of 3.0 ± 1.0 μM and 4.3 ± 1.5 μM respectively. Compound 8v is a competitive inhibitor with respect to pyruvate (Ki = 0.74 μM) and a mixed-type inhibitor with respect to ATP, indicating that it targets the unique carboxyltransferase (CT) domain of PC. Furthermore, compound 8v does not significantly inhibit human carbonic anhydrase II, matrix metalloproteinase-2, malate dehydrogenase or lactate dehydrogenase.
- Burkett, Daniel J.,Wyatt, Brittney N.,Mews, Mallory,Bautista, Anson,Engel, Ryan,Dockendorff, Chris,Donaldson, William A.,St. Maurice, Martin
-
p. 4041 - 4047
(2019/08/26)
-
- Sterically hindered N-aryl/benzyl substituted piperidoimidazolin-2-ylidene palladium complexes and their catalytic activities
-
A series of N-aryl (2a,b) or benzyl (2c,d) substituted piperidoimidazolinium salts and their palladium complexes (3a-d) were prepared and characterized by 1H, 13C NMR, IR spectroscopy and elemental analysis. The crystal structures of 3a and 3c have been determined by X-ray crystallography. Thermogravimetric analysis (TGA) was applied to complexes (3a–d). The palladium complexes have been employed as catalyst for Suzuki-Miyaura cross coupling. The N-aryl substituted complex 3b was a highly efficient precatalyst and successfully employed in Suzuki-Miyaura cross coupling reactions of (hetero)aryl chlorides with arylboronic acids in air. In addition, the oxidative addition step of the reaction mechanism involving chlorobenzene and the catalysts 3a, 3b, 3c and 3d were computationally investigated by the DFT-ω-B97X-D method and complete agreement were obtained with the catalytic results. To measure σ-donating and π-acceptor properties of the new ligands, the rhodium carbonyl complexes were also prepared.
- Gacal, Elif,Denizalt?, Serpil,K?nal, Arma?an,G?k?e, Ayta? Gürhan,Türkmen, Hayati
-
p. 6829 - 6838
(2018/10/20)
-
- Imidazole derivatives [...] and its preparation method (by machine translation)
-
This invention relates to a kind of a kind of [...] imidazole derivatives and method for preparing the same. The structure of this compound is the formula is: . This method is convenient, pervasive, economic. Type I in the organic photoelectric material and based on the analysis of the fluorescence detection has a broad application prospect in the field; in addition, because of such compounds are containing two nitrogen atom heterocyclic compound, has good biological activity, can also be used as a drug intermediate, preparing human, livestock anathematic drug. (by machine translation)
- -
-
Paragraph 0080; 0081
(2016/10/08)
-
- Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites
-
The potential of azaaurones as dual-stage antimalarial agents was investigated by assessing the effect of a small library of azaaurones on the inhibition of liver and intraerythrocytic lifecycle stages of the malaria parasite. The whole series was screened against the blood stage of a chloroquine-resistant Plasmodium falciparum strain and the liver stage of P. berghei, yielding compounds with dual-stage activity and sub-micromolar potency against erythrocytic parasites. Studies with genetically modified parasites, using a phenotypic assay based on the P. falciparum Dd2-ScDHODH line, which expresses yeast dihydroorotate dehydrogenase (DHODH), showed that one of the azaaurone derivatives has the potential to inhibit the parasite mitochondrial electron-transport chain. The global urgency in finding new therapies for malaria, especially against the underexplored liver stage, associated with chemical tractability of azaaurones, warrants further development of this chemotype. Overall, these results emphasize the azaaurone chemotype as a promising scaffold for dual-stage antimalarials.
- Carrasco, Marta P.,Machado, Marta,Gon?alves, Lídia,Sharma, Moni,Gut, Jiri,Lukens, Amanda K.,Wirth, Dyann F.,André, Vania,Duarte, Maria Teresa,Guedes, Rita C.,dos Santos, Daniel J. V. A.,Rosenthal, Philip J.,Mazitschek, Ralph,Prudêncio, Miguel,Moreira, Rui
-
supporting information
p. 2194 - 2204
(2016/10/19)
-
- A general catalyst for Suzuki-Miyaura and Sonogashira reactions of aryl and heteroaryl chlorides in water
-
We report the synthesis of 2-(3-sulfonatomesityl)-5-sulfonatoindenyl) dicyclohexylphosphine hydrate sodium salt and its use in palladium-catalyzed Suzuki-Miyaura and Sonogashira coupling reactions in water (and biphasic water-organic solvent mixtures) to prepare a variety of functionalized biaryls and aryl alkynes in excellent yield. This journal is the Partner Organisations 2014.
- Peng, Hui,Chen, Ya-Qin,Mao, Shu-Lan,Pi, Yun-Xiao,Chen, You,Lian, Ze-Yu,Meng, Tong,Liu, Sheng-Hua,Yu, Guang-Ao
-
supporting information
p. 6944 - 6952
(2014/09/29)
-
- Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists
-
A virtual screening procedure was applied to the discovery of structurally diverse non-steroidal Farnesoid X Receptor (FXR) agonists. From 117 compounds selected by virtual screening, a total of 47 compounds were found to be FXR agonists, with 34 of them showing activity below a concentration of 20 μM. 1H-Pyrazole[3,4-e][1,4]thiazepin-7-one-based hit compound 7 was chosen for hit-to-lead optimization. A large number of 1H-pyrazole[3,4-e][1,4]thiazepin-7- one derivatives was designed, synthesized, and evaluated by a cell-based luciferase transactivation assay for their agonistic activity against FXR. Most of them exhibited low micromolar range of potency and very high efficacy.
- Marinozzi, Maura,Carotti, Andrea,Sansone, Emanuele,MacChiarulo, Antonio,Rosatelli, Emiliano,Sardella, Roccaldo,Natalini, Benedetto,Rizzo, Giovanni,Adorini, Luciano,Passeri, Daniela,De Franco, Francesca,Pruzanski, Mark,Pellicciari, Roberto
-
supporting information; experimental part
p. 3429 - 3445
(2012/07/30)
-
- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-COA DESATURASE
-
The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
- -
-
Page/Page column 19
(2010/07/04)
-
- Palladium/tetraphosphine catalyzed suzuki cross-coupling of heteroarylboronic acids with aryl halides
-
(Chemical Equation Presented) cis,cis,cis-1,2,3,4- Tetrakis(diphenylphosphinomethyl)cyclopentane/[PdCl(C3H 5)]2 efficiently catalyses the Suzuki reaction of heteroarylboronic acids with aryl bromides and also the coupling of arylboronic acids with heteroaryl bromides. The coupling of thiophene- or benzothiopheneboronic acids, furan- or benzofuranboronic acids and 3-pyridineboronic acid with a variety of aryl bromides gave the corresponding coupling products in good yields. However, in most cases, better results in terms of ratio substrate/catalyst were obtained for the reverse reaction using heteroaryl bromides with arylboronic acids.
- Kondolff, Isabelle,Doucet, Henri,Santelli, Maurice
-
p. 109 - 118
(2008/09/18)
-
- Pd-EDTA as an efficient catalyst for Suzuki-Miyaura reactions in water
-
PdCl2-EDTA complex 1 is an efficient catalyst for the Suzuki-Miyaura reactions of aryl and heteroaryl halides with aryl(heteroaryl)boronic acids in water at 20-100°C. Aryl iodides and bromides undergo the cross-coupling with turnover numbers (T
- Korolev, Dmitrii N.,Bumagin, Nikolay A.
-
p. 5751 - 5754
(2007/10/03)
-
- Suzuki coupling reactions of heteroarylboronic acids with aryl halides and arylboronic acids with heteroaryl bromides using a tetraphosphine/palladium catalyst
-
cix,cis,cis-1,2,3,4-Tetrakis(diphenylphosphinomethyl)cyclopentane/ [PdCl(C3H5)]2 efficiently catalyses the Suzuki reaction of heteroarylboronic acids with aryl bromides and also the coupling of arylboronic acids with heteroaryl bromides. The coupling of thiopheneboronic acids, 3-furanboronic acid and 3-pyridineboronic acid with a variety of aryl bromides gave the corresponding adducts in good yields. However, in most cases, better results in terms of substrate/catalyst ratio were obtained for the reaction of heteroaryl bromides with arylboronic acids. Georg Thieme Verlag Stuttgart.
- Kondolff, Isabelle,Doucet, Henri,Santelli, Maurice
-
p. 2057 - 2061
(2007/10/03)
-
- Synthesis of thiophene oligomers via organotin compounds
-
A versatile synthetic route involving the use of organotin compounds has been applied for the preparation of functionalized oligothiophenes. Substituted bithiophenes have been synthesized via the coupling reaction of 2-bromothiophenes with 3-trimethylstannylthiophene. The latter reagent couples with bromoaromatics, bromoheteroaromatics and 2,5-dibromothiophenes to give the corresponding 3-arylthiophenes, 3-heteroarylthiophenes and terthiophenes, respectively. 2-Trimethylstannylthiophene couples with 2,5-dibromo-3-arylthi ophenes to give 3-aryl-α-terthiophenes. The structures of the new compounds were confirmed by elemental analysis, mass spectrometry, 1H- and 13C-NMR spectral data.
- Al-Taweel, Samir A.,Al-Saraierh, Hassan F.
-
-
- The Suzuki-Miyaura cross coupling reactions on solid support. Link to solution phase directed ortho metalation. The Leznoff acetal linker approach to biaryl and heterobiaryl aldehydes
-
The synthesis of the titled compounds by Suzuki-Miyaura cross coupling on Merrifield resin - Leznoff acetal - linked halo benzaldehydes followed by mild acid hydrolysis is reported; synthetic utility for heterocycles based on solution phase Directed ortho Metalation chemistry is demonstrated.
- Chamoin,Houldsworth,Kruse,Bakker, W. Iwema,Snieckus
-
p. 4179 - 4182
(2007/10/03)
-
- Inhibitors of acyl-coA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl)-N'-arylureas
-
A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylurea and related derivatives represented by 2 and 3 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Among these novel compounds, the type 3 series was superior. A pyrazol-3-yl group on the N-benzyl group of this trisubstituted urea (i.e. 3, Ar1 = pyrazol-3- yl) was identified as a heteroaromatic ring providing a good profile of biological activity. As a result of optimization of the combination with the N-alkyl group (R) and N-aryl group (At3), compound 3aq (FR186054) was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irrespective of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicological study revealed compound 3aq to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po.
- Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Sakuma, Yuri,Ishibe, Noriko,Sawada, Masae,Takasugi, Hisashi,Tanaka, Hirokazu
-
p. 2390 - 2410
(2007/10/03)
-