7148-74-5Relevant academic research and scientific papers
Synthesis of functionalized poly(vinyl acetate) mediated by alkyne-terminated RAFT agents
Góis, Joana. R.,Popov, Anatoliy V.,Guliashvili, Tamaz,Serra, Arménio C.,Coelho, Jorge F. J.
, p. 91225 - 91234 (2015)
Two new xanthates with alkyne functionalities were synthesized for the reversible addition fragmentation chain transfer (RAFT) polymerization of vinyl acetate (VAc). The new RAFT agents were fully characterized by 1H and 13C NMR spectroscopy. Unlike the alkyne terminated RAFT agent (AT-X1) the protected alkyne-terminated RAFT agent (PAT-X1) was able to conduct the RAFT polymerization of VAc with a good control over the molecular weight (MW) and relatively narrow MW distributions (n with conversion as well as the close agreement between Mn,th and Mn,GPC values confirmed the controlled features of the RAFT system. It is worth mentioning that the polymer dispersity remained very low (1H NMR, FTIR-ATR and UV-Vis absorption analysis. The "livingness" of the obtained polymer was confirmed by a successful chain extension experiment. The deprotection of the alkyne functionality in the PVAc, allowed a further copper catalyzed azide-alkyne [3 + 2] dipolar cycloaddition reaction (CuAAC) with an azido terminated-poly(ethylene glycol) (PEG-N3), to afford PVAc-PEG block-copolymers as a proof-of-concept.
Synthesis and antimicrobial evaluation of new nitric oxide-donating fluoroquinolone/oxime hybrids
Aziz, Hossameldin A.,Moustafa, Gamal A. I.,Abuo-Rahma, Gamal El-Din A.,Rabea, Safwat M.,Hauk, Glenn,Krishna, Vagolu S.,Sriram, Dharmarajan,Berger, James M.,Abbas, Samar H.
, (2020/10/02)
A new series of nitric oxide-donating fluoroquinolone/oximes was prepared in this study. The nitric oxide release from the prepared compounds was measured using a modified Griess colorimetric method. The antitubercular evaluation of the synthesized compounds indicated that ketone derivatives 2b and 2e and oximes 3b and 3d exhibited somewhat higher activity than their respective parent fluoroquinolones. Mycobacterial DNA cleavage studies and molecular modeling of Mycobacterium tuberculosis DNA gyrase were pursued to explain the observed bioactivity. More important, antibacterial evaluation showed that oximes 3c–e are highly potent against Klebsiella pneumoniae, with minimum inhibitory concentration (MIC) values of 0.06, 0.08, and 0.034 μM, respectively, whereas ketone 2c and oxime 4c are more active against Staphylococcus aureus than ciprofloxacin (MIC values: 0.7, 0.38, and 1.6 μM, respectively). Notably, the antipseudomonal activities of compounds 2a and 4c were much higher than those of their respective parent fluoroquinolones.
Design, synthesis and agricultural evaluation of derivatives of N-Acyl-N-(m-fluoro-benzyl)-6-amino-coumarin
Ding, Yin-hao,Dong, Jing-jing,Feng, Bai-cheng,Hao, Shuang-hong,Jin, Yan,Wei, Yan
supporting information, (2020/08/19)
ABTRACT: This study aims to design and synthesize a series of N-Acyl-N-(m-fluoro- benzyl)-6- amino-coumarins through the principle of active substructure stitching, which are based on the core structure of N-(m-fluoro-benzyl)-6-amino-coumarin. The structures of target compounds e1–e25 have been characterized by 1H NMR, 13C NMR, ESI-MS and elemental analysis. Meanwhile, their agricultural activity have been evaluated in two weeds (Amaranth and Crabgrass) and four widespread noxious pathogens (V.mali, B.cinerea, F.axysporium and C.bacteria). The herbicidal activity results showed that almost all synthetic molecules have a greater impact on the stem system than on the root. Excellent inhibition rates were discovered from compounds e2–e5 and e20–e23 against Amaranth on stems, which were above 58percent(20 mg/L), 68percent(100 mg/L) respectively. Compounds e2 and e21 also exhibited striking inhibition on stems growth of both weeds. Anti-pathogenic activity showed that all the compounds exerted a better inhibitory activity on B.cinerea at 20 ppm compared to control carbendazim. All the heterocyclic substituted compounds (e17–e24, >57percent) made a better influence than the control (54.1percent) at the100 ppm. This research provides promising herbicidal and anti-pathogenic agents that have the better effects and can be potential for further development.
POLYCYCLIC COMPOUND ACTING AS IDO INHIBITOR AND/OR IDO-HDAC DUAL INHIBITOR
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Paragraph 0368-0369, (2020/08/09)
The present invention provides polycyclic compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC. Specifically, the present invention provides compounds represented by the following formula (I), wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an antitumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the antitumor response rate of the antibody and broaden the types of tumors to be treated.
Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists
Deora, Girdhar Singh,Qin, Cheng Xue,Vecchio, Elizabeth A.,Debono, Aaron J.,Priebbenow, Daniel L.,Brady, Ryan M.,Beveridge, Julia,Teguh, Silvia C.,Deo, Minh,May, Lauren T.,Krippner, Guy,Ritchie, Rebecca H.,Baell, Jonathan B.
supporting information, p. 5242 - 5248 (2019/05/28)
Herein we describe the development of a focused series of functionalized pyridazin-3(2H)-one-based formyl peptide receptor (FPR) agonists that demonstrate high potency and biased agonism. The compounds described demonstrated biased activation of prosurvival signaling, ERK1/2 phosphorylation, through diminution of the detrimental FPR1/2-mediated intracellular calcium (Cai2+) mobilization. Compound 50 showed an EC50 of 0.083 μM for phosphorylation of ERK1/2 and an approximate 20-fold bias away from Cai2+ mobilization at the hFPR1.
SPIROCYCLIC COMPOUNDS AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Page/Page column 78, (2019/11/12)
The present invention relates to novel spirocyclic compounds of formulas (1) and (2) which act as modulators of indoleamine 2,3-dioxygenase (ID01) and to the use of said compounds in the prophylaxis and/or treatment of diseases or conditions mediated by indoleamine 2,3-dioxygenase. The invention further relates to pharmaceutical compositions comprising the novel compounds.
Iron-Catalyzed Intramolecular C-H Amination of α-Azidyl Amides
Zhao, Xiaopeng,Liang, Siyu,Fan, Xing,Yang, Tonghao,Yu, Wei
supporting information, p. 1559 - 1563 (2019/03/20)
Iron-catalyzed intramolecular C-H amination of aliphatic azides has recently emerged as a powerful tool for the preparation of nitrogen heterocycles. This paper reports that α-azidyl amides can be converted in high efficacy to imidazolinone compounds via intramolecular C(sp3)-H amination by the action of a simple catalytic system composed of FeCl2 and a β-diketiminate ligand. The reactions provide a simple and atom-economical approach toward polysubstituted imidazolinones.
Method and using tracer charged ion channel
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Paragraph 0227; 0229; 0230-0232, (2018/08/20)
The invention provides compounds, compositions, methods, and kits for the treatment of pain, itch, and neurogenic inflammation.
Method for manufacturing isavuconazole or ravuconazole
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Paragraph 0072; 0073, (2017/08/27)
The invention provides a method for manufacturing a triazole compound isavuconazole or ravuconazole which is enriched by a diastereoisomer and enantiomer. The method comprises the following steps: a Reformatsky reaction is carried out between ketone and dihalogeno metal propionitrile; an enantiomer mixture is generated, and separation is carried out. The method can obviously reduce steps for synthesis of isavuconazole or ravuconazole, yield of products is improved, and production cost is reduced.
Transition-Metal-Free Coupling of Alkynes with α-Bromo Carbonyl Compounds: An Efficient Approach towards β,γ-Alkynoates and Allenoates
Liu, Wenbo,Chen, Zhengwang,Li, Lu,Wang, Haining,Li, Chao-Jun
supporting information, p. 5888 - 5893 (2016/04/26)
A direct transition-metal-free coupling between alkynes and α-bromo carbonyl compounds has been developed with ultraviolet (UV) light in aqueous media. This method represents a facile approach to synthetically useful β,γ-alkynyl esters and amides stereoselectively from two readily available starting materials. As an example of the synthetic application of the products, the alkynyl esters were readily converted into allenoates. Time for UV! A direct coupling between alkynes and α-bromo compounds has been developed with ultraviolet light in aqueous media (see scheme). This method represents a facile approach to synthetically useful β,γ-alkynyl esters and amides stereoselectively from two readily available starting materials.
