Month: October 2022

Morimoto, Mariko; Cao, Wendy; Bergman, Robert G.; Raymond, Kenneth N.; Toste, F. Dean published an article on February 3 ,2021. The article was titled 《Chemoselective and Site-Selective Reductions Catalyzed by a Supramolecular Host and a Pyridine-Borane Cofactor》, and you may find the article in Journal of the American Chemical Society.Recommanded Product: 2418-95-3 The information in the text is summarized as follows:

Supramol. catalysts emulate the mechanism of enzymes to achieve large rate accelerations and precise selectivity under mild and aqueous conditions. While significant strides have been made in the supramol. host-promoted synthesis of small mols., applications of this reactivity to chemoselective and site-selective modification of complex biomols. remain virtually unexplored. We report here a supramol. system where coencapsulation of pyridine-borane with a variety of mols. including enones, ketones, aldehydes, oximes, hydrazones, and imines effects efficient reductions under basic aqueous conditions. Upon subjecting unprotected lysine to the host-mediated reductive amination conditions, we observed excellent ε-selectivity, indicating that differential guest binding within the same mol. is possible without sacrificing reactivity. Inspired by the post-translational modification of complex biomols. by enzymic systems, we then applied this supramol. reaction to the site-selective labeling of a single lysine residue in an 11-amino acid peptide chain and human insulin. In addition to this study using H-Lys(Boc)-OH, there are many other studies that have used H-Lys(Boc)-OH(cas: 2418-95-3Recommanded Product: 2418-95-3) was used in this study.

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. In addition to subunits of proteins, amino acids have many other functions as well, including osmoregulation (proline), neurotransmitters (gamma-aminobutyric acid), metabolic intermediates (ornithine and citrulline), and inhibitors (dehydroproline).Recommanded Product: 2418-95-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2016,Chan, Jessica Z.; Yao, Wenzhi; Hastings, Brian T.; Lok, Charles K.; Wasa, Masayuki published 《Direct Mannich-Type Reactions Promoted by Frustrated Lewis Acid/Bronsted Base Catalysts》.Angewandte Chemie, International Edition published the findings.COA of Formula: C4H9NO2 The information in the text is summarized as follows:

Direct Mannich-type reactions that afford both α- and β-amino esters by the reaction of a broad range of carbonyl compounds and aldimines are disclosed. The transformation is promoted by a sterically frustrated Lewis acid/Bronsted base pair, which is proposed to operate cooperatively: Within the catalyst complex, an enolate is generated that then reacts with a hydrogen-bond-activated imine. Noncovalent interactions between reactants and the catalyst provide selectivity and new opportunities for future catalyst design.N-Methoxy-N-methylacetamide(cas: 78191-00-1COA of Formula: C4H9NO2) was used in this study.

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.COA of Formula: C4H9NO2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2016,Batrice, Rami J.; Kefalidis, Christos E.; Maron, Laurent; Eisen, Moris S. published 《Actinide-Catalyzed Intermolecular Addition of Alcohols to Carbodiimides》.Journal of the American Chemical Society published the findings.Reference of tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:

The unprecedented actinide-catalyzed addition of alcs. to carbodiimides is presented. This represents a rare example of thorium-catalyzed transformations of an alc. substrate and the first example of uranium complexes showing catalytic reactivity with alcs. Using the uranium and thorium amides U[N(SiMe3)2]3 and [(Me3Si)2N]2An[κ2-(N,C)-CH2Si(CH3)2N(SiMe3)] (An = Th or U), alc. additions to unsaturated carbon-nitrogen bonds are achieved in short reaction times with excellent selectivities and high to excellent yields. Computational studies, supported by exptl. thermodn. data, suggest plausible models of the profile of the reaction which allow the system to overcome the high barrier of scission of the actinide-oxygen bond. Accompanied by exptl. determined kinetic parameters, a plausible mechanism is proposed for the catalytic cycle. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Reference of tert-Butyl N,N’-diisopropylcarbamimidate)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Reference of tert-Butyl N,N’-diisopropylcarbamimidate

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2018,Imberdis, Arnaud; Lefevre, Guillaume; Thuery, Pierre; Cantat, Thibault published 《Metal-Free and Alkali-Metal-Catalyzed Synthesis of Isoureas from Alcohols and Carbodiimides》.Angewandte Chemie, International Edition published the findings.Application In Synthesis of tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:

The first addition of alcs. to carbodiimides catalyzed by transition-metal-free compounds employs 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and its alkali metal salts. Isoureas were obtained in short reaction times and high yields when TBDK was used as the catalyst. Control of the coordination sphere of potassium with exogenous chelating ligands, in combination with mechanistic DFT calculations, demonstrated the role and pos. influence of the alkali-metal cation on the kinetics. In the experiment, the researchers used many compounds, for example, tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Application In Synthesis of tert-Butyl N,N’-diisopropylcarbamimidate)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Application In Synthesis of tert-Butyl N,N’-diisopropylcarbamimidate

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《The effect of substituted benzene-sulfonamides and clinically licensed drugs on the catalytic activity of CynT2, a carbonic anhydrase crucial for Escherichia coli life cycle》 was published in International Journal of Molecular Sciences in 2020. These research results belong to Del Prete, Sonia; De Luca, Viviana; Bua, Silvia; Nocentini, Alessio; Carginale, Vincenzo; Supuran, Claudiu T.; Capasso, Clemente. Related Products of 70-55-3 The article mentions the following:

Proteins are relevant antimicrobial drug targets, and among them, enzymes represent a significant group, since most of them catalyze reactions essential for supporting the central metabolism, or are necessary for the pathogen vitality. Genomic exploration of pathogenic and non-pathogenic microorganisms has revealed genes encoding for a superfamily of metalloenzymes, known as carbonic anhydrases (CAs, EC 4.2.1.1). CAs catalyze the physiol. crucial reversible reaction of the carbon dioxide hydration to bicarbonate and protons. Herein, we investigated the sulfonamide inhibition profile of the recombinant β-CA (CynT2) identified in the genome of the Gram-neg. bacterium Escherichia coli. This biocatalyst is indispensable for the growth of the microbe at atm. pCO2. Surprisingly, this enzyme has not been investigated for its inhibition with any class of CA inhibitors. Here, we show that CynT2 was strongly inhibited by some substituted benzene-sulfonamides and the clin. used inhibitor sulpiride (KIs in the range of 82-97 nM). This study may be relevant for identifying novel CA inhibitors, as well as for another essential part of the drug discovery pipeline, such as the structure-activity relationship for this class of enzyme inhibitors. In the experimental materials used by the author, we found 4-Methylbenzenesulfonamide(cas: 70-55-3Related Products of 70-55-3)

4-Methylbenzenesulfonamide(cas: 70-55-3) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Related Products of 70-55-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype》 was published in Bioorganic & Medicinal Chemistry Letters in 2020. These research results belong to Temple, Kayla J.; Engers, Julie L.; Long, Madeline F.; Watson, Katherine J.; Chang, Sichen; Luscombe, Vincent B.; Jenkins, Matthew T.; Rodriguez, Alice L.; Niswender, Colleen M.; Bridges, Thomas M.; Jeffrey Conn, P.; Engers, Darren W.; Lindsley, Craig W.. Name: N-Methoxy-N-methylacetamide The article mentions the following:

This Letter details the authors’ efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, the authors studied a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration. In the part of experimental materials, we found many familiar compounds, such as N-Methoxy-N-methylacetamide(cas: 78191-00-1Name: N-Methoxy-N-methylacetamide)

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Name: N-Methoxy-N-methylacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《Preclinical development of FA5, a novel AMP-activated protein kinase (AMPK) activator as an innovative drug for the management of bowel inflammation》 was written by Antonioli, Luca; Pellegrini, Carolina; Fornai, Matteo; Benvenuti, Laura; D’Antongiovanni, Vanessa; Colucci, Rocchina; Bertani, Lorenzo; Salvo, Clelia Di; Semeghini, Giorgia; La Motta, Concettina; Giusti, Laura; Zallocco, Lorenzo; Ronci, Maurizio; Quattrini, Luca; Angelucci, Francesco; Coviello, Vito; Oh, Won-Keun; Ha, Quy Thi Kim; Nemeth, Zoltan H.; Hasko, Gyorgy; Blandizzi, Corrado. Synthetic Route of C2H4BrNO And the article was included in International Journal of Molecular Sciences in 2021. The article conveys some information:

Acadesine (ACA), a pharmacol. activator of AMP-activated protein kinase (AMPK), showed a promising beneficial effect in a mouse model of colitis, indicating this drug as an alternative tool to manage IBDs. However, ACA displays some pharmacodynamic limitations precluding its therapeutical applications. Our study was aimed at evaluating the in vitro and in vivo effects of FA-5 (a novel direct AMPK activator synthesized in our laboratories) in an exptl. model of colitis in rats. A set of experiments evaluated the ability of FA5 to activate AMPK and to compare the efficacy of FA5 with ACA in an exptl. model of colitis. The effects of FA-5, ACA, or dexamethasone were tested in rats with 2,4-dinitrobenzenesulfonic acid (DNBS)-induced colitis to assess systemic and tissue inflammatory parameters. In in vitro experiments, FA5 induced phosphorylation, and thus the activation, of AMPK, contextually to the activation of SIRT-1. In vivo, FA5 counteracted the increase in spleen weight, improved the colon length, ameliorated macroscopic damage score, and reduced TNF and MDA tissue levels in DNBS-treated rats. Of note, FA-5 displayed an increased anti-inflammatory efficacy as compared with ACA. The novel AMPK activator FA-5 displays an improved anti-inflammatory efficacy representing a promising pharmacol. tool against bowel inflammation. The experimental part of the paper was very detailed, including the reaction process of 2-Bromoacetamide(cas: 683-57-8Synthetic Route of C2H4BrNO)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Synthetic Route of C2H4BrNO

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

De Luca, Viviana; Angeli, Andrea; Mazzone, Valeria; Adelfio, Claudia; Carta, Fabrizio; Selleri, Silvia; Carginale, Vincenzo; Scaloni, Andrea; Supuran, Claudiu T.; Capasso, Clemente published an article in 2021. The article was titled 《Inhibitory Effects of Sulfonamide Derivatives on the β-Carbonic Anhydrase (MpaCA) from Malassezia pachydermatis, a Commensal, Pathogenic Fungus Present in Domestic Animals》, and you may find the article in International Journal of Molecular Sciences.Computed Properties of C7H9NO2S The information in the text is summarized as follows:

Fungi are exposed to various environmental variables during their life cycle, including changes in CO2 concentration CO2 has the potential to act as an activator of several cell signaling pathways. In fungi, the sensing of CO2 triggers cell differentiation and the biosynthesis of proteins involved in the metabolism and pathogenicity of these microorganisms. The mol. machineries involved in CO2 sensing constitute a promising target for the development of antifungals. Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial enzymes in the CO2 sensing systems of fungi, because they catalyze the reversible hydration of CO2 to proton and HCO3-. Bicarbonate in turn boots a cascade of reactions triggering fungal pathogenicity and metabolism Accordingly, CAs affect microorganism proliferation and may represent a potential therapeutic target against fungal infection. Here, the inhibition of the unique β-CA (MpaCA) encoded in the genome of Malassezia pachydermatis, a fungus with substantial relevance in veterinary and medical sciences, was investigated using a series of conventional CA inhibitors (CAIs), namely aromatic and heterocyclic sulfonamides. This study aimed to describe novel candidates that can kill this harmful fungus by inhibiting their CA, and thus lead to effective anti-dandruff and anti-seborrheic dermatitis agents. In this context, current antifungal compounds, such as the azoles and their derivatives, have been demonstrated to induce the selection of resistant fungal strains and lose therapeutic efficacy, which might be restored by the concomitant use of alternative compounds, such as the fungal CA inhibitors. In addition to this study using 4-Methylbenzenesulfonamide, there are many other studies that have used 4-Methylbenzenesulfonamide(cas: 70-55-3Computed Properties of C7H9NO2S) was used in this study.

4-Methylbenzenesulfonamide(cas: 70-55-3) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Computed Properties of C7H9NO2S

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Category: amides-buliding-blocksIn 2021 ,《Synthesis and Applications of Polysubstituted Bicyclo[1.1.0]butanes》 appeared in Journal of the American Chemical Society. The author of the article were McNamee, Ryan E.; Thompson, Amber L.; Anderson, Edward A.. The article conveys some information:

The synthesis of tri- and tetrasubstituted bicyclo[1.1.0]butanes (BCBs) via directed metalation of readily accessed BCB amides is reported. This straightforward “”late stage”” approach generates a wide variety of bridge-substituted BCBs that was easily converted into other useful small ring building blocks. Access to a monodeuterated BCB provides an unprecedented insight into the mechanism of dihalocarbene insertion into BCBs to afford bicyclo[1.1.1]pentanes. In the experiment, the researchers used N-Methoxy-N-methylacetamide(cas: 78191-00-1Category: amides-buliding-blocks)

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Formula: C4H9NO2In 2018 ,《Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Tummalapalli, Sreedhar R.; Bhat, Rohit; Chojnowski, Agnieszka; Prorok, Monika; Kreiss, Tamara; Goldberg, Ronald; Canan, Stacie; Hawryluk, Natalie; Mortensen, Deborah; Khetani, Vikram; Zeldis, Jerome; Siekierka, John J.; Rotella, David P.. The article conveys some information:

Lymphatic filariasis infects over 120 million people worldwide and can lead to significant disfigurement and disease. Resistance is emerging with current treatments, and these therapies have dose limiting adverse events; consequently new targets are needed. One approach to achieve this goal is inhibition of parasitic protein kinases involved in circumventing host defense mechanisms. This report describes structure-activity relationships leading to the identification of a potent, orally bioavailable stress activated protein kinase inhibitor that may be used to investigate this hypothesis.N-Methoxy-N-methylacetamide(cas: 78191-00-1Formula: C4H9NO2) was used in this study.

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Formula: C4H9NO2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics