160706-61-6Relevant articles and documents
New azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study
Maccallini, Cristina,Gallorini, Marialucia,Sisto, Francesca,Akdemir, Atilla,Ammazzalorso, Alessandra,De Filippis, Barbara,Fantacuzzi, Marialuigia,Giampietro, Letizia,Carradori, Simone,Cataldi, Amelia,Amoroso, Rosa
, p. 1632 - 1645 (2021)
Nonsteroidal aromatase inhibitors (NSAIs) are well-established drugs for the therapy of breast cancer. However, they display some serious side effects, and their efficacy can be compromised by the development of chemoresistance. Previously, we have report
A novel class of potent γ-aminobutyric acid aminotransferase inhibitor, 3-(hydroxyamino)propylamine and analogues
Fushiya, Shinji,Kanazawa, Toshiyuki,Nozoe, Shigeo
, p. 2089 - 2094 (1997)
Hydroxyamino analogues of γ-aminobutyric acid (GABA) were synthesized and evaluated for inhibitory activity toward γ-aminobutyric acid aminotransferase (GABA-T). The title compound, 3-(hydroxyamino)propylamine (HPA), showed a potent inhibitory activity. The inhibition is competitive with respect to GABA and the K(i) value of GABA-T for HPA is 0.4 mmol. The activity of inhibition is comparable to those of aminoxyacetic acid and valproic acid. 3-(Hydroxyaminomethyl)piperidine (3HMP), a cyclic analogue of HPA, also showed a patent inhibitory activity, whereas 3-(methoxyamino)propylamine (OMe-HPA), 3-(N-hydroxy-N-methylamino)propylamine (NMe-HPA) and 4-(hydroxyamino)piperidine (4HP) showed weak activity.
Method of fluorination using iodonium ylides
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Page/Page column 60-61, (2019/04/30)
A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
Manganese Catalyzed Hydrogenation of Enantiomerically Pure Esters
Widegren, Magnus B.,Clarke, Matthew L.
supporting information, p. 2654 - 2658 (2018/05/17)
A manganese-catalyzed hydrogenation of esters has been accomplished with TONs up to 1000, using cheap, environmentally benign, potassium carbonate and simple alcohols as activator and solvent, respectively. The weakly basic conditions lead to good functional group tolerance and enable the hydrogenation of enantiomerically enriched α-chiral esters with essentially no loss of stereochemical integrity.
AZOLE-SUBSTITUTED PYRIDINE COMPOUND
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Paragraph 0636; 0637; 0638, (2019/01/08)
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, wherein the structure represented by formula [III] shown below represents any of the structures represented by formula group [IV] shown below, wherein R1 represents a hydrogen atom, a fluorine atom, methyl, etc.; R2, R3, and R4 each independently represent a hydrogen atom, a fluorine atom, or methyl; W represents a single bond, C1-3alkanediyl, or the formula -O-CH2CH2-; and ring A represents (a) substituted C4-6cycloalkyl, (b) substituted 4- to 6-membered saturated nitrogen-containing heterocyclyl, (c) substituted phenyl, (d) substituted pyridyl, (e) substituted 2,3-dihydrobenzofuran, (f) 4- to 6-membered saturated oxygen-containing heterocyclyl, etc.
Carbazole inhibitors of histamine receptors for the treatment of disease
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, (2012/01/04)
The present invention relates to carbazole compounds, pharmaceutical compositions comprising them, and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
Potent inhibition of Norwalk virus by cyclic sulfamide derivatives
Dou, Dengfeng,Tiew, Kok-Chuan,He, Guijia,Mandadapu, Sivakoteswara Rao,Aravapalli, Sridhar,Alliston, Kevin R.,Kim, Yunjeong,Chang, Kyeong-Ok,Groutas, William C.
experimental part, p. 5975 - 5983 (2011/11/07)
A new class of compounds that exhibit anti-norovirus activity in a cell-based system and embody in their structure a cyclosulfamide scaffold has been identified. The structure of the initial hit (compound 2a, ED50 4 μM, TD50 50 μM) has been prospected by exploiting multiple points of diversity and generating appropriate structure-activity relationships.
A library of conformationally restricted saturated heterocyclic sulfonyl chlorides
Zhersh, Sergey,Buryanov, Volodymyr V.,Karpenko, Oleksandr V.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
scheme or table, p. 3669 - 3674 (2011/12/16)
An approach to the synthesis of conformationally restricted saturated heterocyclic sulfonyl chlorides is described. Being guided by the principle of diversity-oriented conformational restriction, a mini-library of saturated heterocyclic sulfonyl chlorides
10-Substituted Cytisine Derivatives and Methods of Use Thereof
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Page/Page column 32, (2010/03/31)
The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is subs
NOVEL CYCLIC AMINOBENZOIC ACID DERIVATIVE
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Page/Page column 51, (2010/11/27)
The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or - (CH2)n- (n represents 0,1 or 2) ; X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and -COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.