39969-56-7Relevant articles and documents
Multibranched Calix[4]arene-Based Sensitizers for Efficient Photocatalytic Hydrogen Production
Abbotto, Alessandro,Baldini, Laura,Boldrini, Chiara Liliana,Decavoli, Cristina,Dolla, Tarekegn Heliso,Faroldi, Federica,Fornasiero, Paolo,Manfredi, Norberto,Montini, Tiziano,Sansone, Francesco
, p. 284 - 288 (2021)
In the field of direct production of hydrogen from solar energy and water, photocatalytic methods hold great potential especially when metal-free molecular components are preferred. In this work, we have developed a new class of calix[4]arene-based molecu
Synthesis, evaluation and in silico studies of novel BRD4 bromodomain inhibitors bearing a benzo[d]isoxazol scaffold
Zhang, Maofeng,Liu, Zhuyun,Wang, Lizhong,Li, Yan,Ma, Yonggang
, (2021/02/12)
Abstract: The BRD4 protein is associated with various diseases, which has been an attractive target for the treatment of cancer and inflammation. This paper is a follow-up to our previous studies, in which we report the structure-based design, synthesis, and evaluation of a new class of small-molecule BRD4 bromodomain inhibitors bearing a benzo[d]isoxazol scaffold. The SARs focused on exploration of the 2′ or 3′ position to afford novel inhibitors that may avoid potential metabolically unstable site. The most potent inhibitor 13f exhibited high binding affinity to BRD4(1) with a ΔTm value of 7.8 °C as evaluated in thermal shift assay (TSA). The potent activity was also demonstrated by a peptide competition assay with an IC50 value of 0.21?μM. The docking studies revealed the binding mode of the compounds with the active site of BRD4(1). In addition, in silico predictions indicated that these compounds possessed good drug-likeness and pharmacokinetic profile. Graphic abstract: This paper is a follow-up to our previous studies, in which we report the structure-based design,synthesis, and evaluation of a new class of small-molecule BRD4 bromodomain inhibitors bearing a benzo[d]isoxazolscaffold.[Figure not available: see fulltext.].
GLP-1 RECEPTOR MODULATORS
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Paragraph 001027, (2016/06/28)
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where "^^^^" represents either or both the R and S form of the compound) (I) where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
Continuous flow reduction of artemisinic acid utilizing multi-injection strategies - Closing the gap towards a fully continuous synthesis of antimalarial drugs
Pieber, Bartholom?us,Glasnov, Toma,Kappe, C. Oliver
supporting information, p. 4368 - 4376 (2015/03/14)
One of the rare alternative reagents for the reduction of carbon-carbon double bonds is diimide (HN=NH), which can be generated in situ from hydrazine hydrate (N2H4·H2O) and O2. Although this selective method is extremely clean and powerful, it is rarely used, as the rate-determining oxidation of hydrazine in the absence of a catalyst is relatively slow using conventional batch protocols. A continuous high-temperature/high-pressure methodology dramatically enhances the initial oxidation step, at the same time allowing for a safe and scalable processing of the hazardous reaction mixture. Simple alkenes can be selectively reduced within 10-20 min at 100-120°C and 20 bar O2 pressure. The development of a multi-injection reactor platform for the periodic addition of N2H4·H2O enables the reduction of less reactive olefins even at lower reaction temperatures. This concept was utilized for the highly selective reduction of artemisinic acid to dihydroartemisinic acid, the precursor molecule for the semisynthesis of the antimalarial drug artemisinin. The industrially relevant reduction was achieved by using four consecutive liquid feeds (of N2H4·H2O) and residence time units resulting in a highly selective reduction within approximately 40 min at 60°C and 20 bar O2 pressure, providing dihydroartemisinic acid in ≥93% yield and ≥95% selectivity.
Novel biphenyl-3-carboxamide derivatives or salt thereof and pharmaceutical composition for treating or preventing autoimmune diseases comprising the same
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Paragraph 0034; 0058; 0060-0064, (2021/10/21)
The present invention refers to novel biphenyl-3-carboxamide amide derivatives or a salt thereof and a self effect because of having immunosuppressive effect and the treatment of auto-immune diseases in relates to pharmaceutical compositions for the treat
Photodriven Transfer Hydrogenation of Olefins
Leow, Dasheng,Chen, Ying-Ho,Hung, Tzu-Hang,Su, Ying,Lin, Yi-Zhen
supporting information, p. 7347 - 7352 (2016/02/18)
An improved practical method for the photodriven diimide reduction of olefins was investigated. This catalyst-free procedure proceeds at ambient temperature, utilizes air as oxidant and a lower hydrazine loading, and produces inert nitrogen gas as the sole byproduct. Several functional groups were tolerated, and in some cases, the reaction was chemoselective. Challenging substrates such as cinnamate ester derivatives and trans-stilbene were reduced in excellent yields. The small amount of UVA rays emitted from a household compact fluorescent light bulb was proposed to enable the cis/trans isomerization of the diimide and to promote the loss of hydrogen from the diimide.
In situ generation of diimide from hydrazine and oxygen: Continuous-flow transfer hydrogenation of olefins
Pieber, Bartholomaeus,Martinez, Sabrina Teixeira,Cantillo, David,Kappe, C. Oliver
supporting information, p. 10241 - 10244 (2013/10/21)
No catalyst required! A highly efficient, catalyst-free process to generate diimide in situ from hydrazine monohydrate and molecular oxygen for the selective reduction of alkenes has been developed. The use of a gas-liquid segmented flow system allowed safe operating conditions and dramatically enhanced this atom-economical reaction, resulting in short processing times. Copyright
Guanidine catalyzed aerobic reduction: A selective aerobic hydrogenation of olefins using aqueous hydrazine
Lamani, Manjunath,Guralamata, Ravikumara Siddappa,Prabhu, Kandikere Ramaiah
supporting information; experimental part, p. 6583 - 6585 (2012/07/14)
An efficient aerobic reduction of olefins, internal as well as terminal, is developed using guanidine as an organocatalyst. A remarkable chemoselectivity in reduction has been demonstrated in the presence of a variety of functional groups and protective groups and a selective reduction of a terminal olefin in the presence of an internal olefin is revealed.
Iron(III) chloride-catalysed aerobic reduction of olefins using aqueous hydrazine at ambient temperature
Lamani, Manjunath,Ravikumara, Guralamata S.,Prabhu, Kandikere Ramaiah
supporting information; experimental part, p. 1437 - 1442 (2012/07/03)
A chemoselective reduction of olefins and acetylenes is demonstrated by employing catalytic amounts of ferric chloride hexahydrate (FeCl 3·6 H2O) and aqueous hydrazine (NH 2NH2·H2O) as hydrogen source at room temperature. The reduction is chemoselective and tolerates a variety of reducible functional groups. Unlike other metal-catalysed reduction methods, the present method employs a minimum amount of aqueous hydrazine (1.5-2 equiv.). Also, the scope of this method is demonstrated in the synthesis of ibuprofen in aqueous medium. Copyright
Small molecules that regulate zymosan phagocytosis of macrophage through deactivation of Rho GTPases
Bang, Joon Seok,Kim, Young Jin,Song, Jiho,Yoo, Jong-Sun,Lee, Seul,Lee, Mi Ji,Min, Hyeyoung,Hwang, Kwang Woo,Min, Kyung Hoon
, p. 5262 - 5268 (2012/11/07)
Phagocytosis and subsequent degradation of pathogens by macrophages play a pivotal role in host innate immune response to microbial infections. To find small molecule regulators for the investigation of complicated phagocytic process, we screened our in-h
