Tag: 100-200

In 2016,Fernandez, Jorge; Chicharro, Jesus; Bueno, Jose M.; Lorenzo, Milagros published 《Isoxazole mediated synthesis of 4-(1H)pyridones: improved preparation of antimalarial candidate GSK932121》.Chemical Communications (Cambridge, United Kingdom) published the findings.Formula: C4H9NO2 The information in the text is summarized as follows:

A new synthesis of the antimalarial clin. candidate GSK932121 is described. This approach has two key reactions, the selective acylation of an unprotected 3-hydroxymethyl-5-Me isoxazole and the reductive N-O bond cleavage of the previously functionalized isoxazole derivative, to give the 4-(1H)pyridone ring present in the final structure. The complete synthesis consists of 5 steps (vs. 10 steps in previously published reports) and has enabled the preparation of the material in kilogram scale to support clin. studies. The experimental part of the paper was very detailed, including the reaction process of N-Methoxy-N-methylacetamide(cas: 78191-00-1Formula: C4H9NO2)

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Formula: C4H9NO2

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

《Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania》 was written by Medeiros, Andrea; Benitez, Diego; Korn, Ricarda S.; Ferreira, Vinicius C.; Barrera, Exequiel; Carrion, Federico; Pritsch, Otto; Pantano, Sergio; Kunick, Conrad; de Oliveira, Camila I.; Orban, Oliver C. F.; Comini, Marcelo A.. Safety of 2-BromoacetamideThis research focused ontrypanothione synthetase inhibition binding mode mol interaction Leishmania; Leishmania; Paullone; inhibition mode; thiol; trypanothione synthetase. The article conveys some information:

Trypanothione synthetase (TryS) produces N1,N8-bis(glutathionyl)spermidine (or trypanothione) at the expense of ATP. Trypanothione is a metabolite unique and essential for survival and drug-resistance of trypanosomatid parasites. In this study, we report the mechanistic and biol. characterization of optimized N5-substituted paullone analogs with anti-TryS activity. Several of the new derivatives retained submicromolar IC50 against leishmanial TryS. The binding mode to TryS of the most potent paullones has been revealed by means of kinetic, biophys. and mol. modeling approaches. A subset of analogs showed an improved potency (EC50 0.5-10μM) and selectivity (20-35) against the clin. relevant stage of Leishmania braziliensis (mucocutaneous leishmaniasis) and L. infantum (visceral leishmaniasis). For a selected derivative, the mode of action involved intracellular depletion of trypanothione. Our findings shed light on the mol. interaction of TryS with rationally designed inhibitors and disclose a new set of compounds with on-target activity against different Leishmania species. In addition to this study using 2-Bromoacetamide, there are many other studies that have used 2-Bromoacetamide(cas: 683-57-8Safety of 2-Bromoacetamide) was used in this study.

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.Safety of 2-Bromoacetamide

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

Computed Properties of C4H9NO2In 2016 ,《Screening of new antileukemic agents from essential oils of algae extracts and computational modeling of their interactions with intracellular signaling nodes》 was published in European Journal of Pharmaceutical Sciences. The article was written by Atasever-Arslan, Belkis; Yilancioglu, Kaan; Kalkan, Zeynep; Timucin, Ahmet Can; Gur, Hazal; Isik, Fatma Busra; Deniz, Emre; Erman, Batu; Cetiner, Selim. The article contains the following contents:

Microalgae are very rich in bioactive compounds, minerals, polysaccharides, poly-unsaturated fatty acids and vitamins, and these rich constituents make microalgae an important resource for the discovery of new bioactive compounds with applications in biotechnol. In this study, we studied the antileukemic activity of several chosen microalgae species at the mol. level and assessed their potential for drug development. Here we identified Stichococcus bacillaris, Phaeodactylum tricornutum, Microcystis aeruginosa and Nannochloropsis oculata microalgae extracts with possible antileukemic agent potentials. Specifically we studied the effects of these extracts on intracellular signal nodes and apoptotic pathways. We characterized the composition of essential oils of these fifteen different algae extracts using gas chromatog.-mass spectrometry (GC-MS). Finally, to identify potential mol. targets causing the phenotypic changes in leukemic cell lines, we docked a selected group of these essential oils to several key intracellular proteins. According to results of rank score algorithm, five of these essential oils analyzed might be considered as in silico plausible candidates to be used as antileukemic agents. The results came from multiple reactions, including the reaction of N-Methoxy-N-methylacetamide(cas: 78191-00-1Computed Properties of C4H9NO2)

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Computed Properties of C4H9NO2

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

Application In Synthesis of N-Methoxy-N-methylacetamideIn 2020 ,《Oral administration of royal jelly may improve the preservation of rooster spermatozoa》 was published in Journal of Animal Physiology and Animal Nutrition. The article was written by Rahnama, Golsomeh; Deldar, Hamid; Ansari Pirsaraei, Zarbakht; Kazemifard, Mohammad. The article contains the following contents:

The aim of the present study was to investigate the effect of dietary supplementation of royal jelly (RJ) on liquid and frozen storage of rooster spermatozoa. Twenty-five 30-wk-old of Mazandaran native breeder roosters were randomly divided into five treatments (n = 5 roosters/group). Exptl. treatments are designed to include a control group and various levels (0.0 (RJ0), 100 (RJ100), 200 (RJ200), 300 (RJ300) mg kg-1 BW-1) of royal jelly (RJ) that were fed to the roosters using force-feed method. The result of this study showed that the spermatozoa forward progressive motility, abnormality, membrane integrity, and viability were improved by the RJ100 group compared to the other groups after 24 and 48 h storage period at 4°C. The percentage of membrane integrity and forward progressive motility after freeze-thawing in the RJ100 group was significantly higher than the other groups, and the percentage of abnormal spermatozoa was lower. A significant decrease in semen quality parameters was seen after 24 and 48 h of refrigeration, but there was no observed change between 2 and 24 h in the RJ100. Moreover, after freeze-thawing, DNA integrity and mitochondrial activity in the RJ100 group were significantly higher than the other groups. According to our results, feeding of RJ at 100 mg kg-1 BW-1 to the roosters was improved spermatozoa characteristics during liquid and cryopreservation conditions. In the experiment, the researchers used N-Methoxy-N-methylacetamide(cas: 78191-00-1Application In Synthesis of 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.Application In Synthesis of N-Methoxy-N-methylacetamide

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

Synthetic Route of C7H9NO2SIn 2020 ,《Au(I)/Au(III)-Catalyzed C-N coupling》 appeared in Chemical Communications (Cambridge, United Kingdom). The author of the article were Rodriguez, Jessica; Adet, Nicolas; Saffon-Merceron, Nathalie; Bourissou, Didier. The article conveys some information:

Cycling between Au(I) and Au(III) is challenging, so gold-catalyzed cross-couplings are rare. The (MeDalphos)AuCl complex, which the authors showed was prone to undergo oxidative addition, is reported here to efficiently catalyze the C-N coupling of aryl iodides and amines. The transformation does not require an external oxidant or a directing group. It is robust and works with a wide scope of aryl iodides and N-nucleophiles under mild conditions. Mechanistic studies, including the NMR and MS characterization of a key aryl amido Au(III) complex, strongly support a 2e redox cycle in which oxidative addition precedes transmetalation and reductive elimination is the rate-determining step.4-Methylbenzenesulfonamide(cas: 70-55-3Synthetic Route of C7H9NO2S) was used in this study.

4-Methylbenzenesulfonamide(cas: 70-55-3) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Synthetic Route of C7H9NO2S

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

The author of 《Simultaneous infrared-ultrasound irradiation in organic synthesis: acylation of amines alcohols and amino alcohols》 were Luna-Mora, Ricardo Alfredo; Ortega-Jimenez, Fernando; Rios-Guerra, Hulme; Garcia-Estrada, Jose Guadalupe; Perez-Flores, Francisco Javier; Gonzalez-Carrillo, Jessica; Torres-Reyes, Angeles; Moreno-Gonzalez, Linda; Martinez-Zaldivar, Alejandro; Penieres-Carrillo, Jose Guillermo. And the article was published in Journal of the Mexican Chemical Society in 2019. Product Details of 70298-88-3 The author mentioned the following in the article:

The acylation of both aliphatic and aromatic amines, alcs. and amino alcs. by simultaneous IR-ultrasound irradiation (SIUI) in solvent-free conditions in short reaction times and with good to excellent yields was achieved. The results obtained with SIUI and for thermal, IR and ultrasound energy sources are compared. This is the first report regarding to the application of SIUI in acylation reactions. In the part of experimental materials, we found many familiar compounds, such as 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Product Details of 70298-88-3)

2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Product Details of 70298-88-3

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

《Kinetics and mechanism of reversible, base-catalyzed ring closure of 3-(methoxycarbonyl)propionanilide and (methoxycarbonyl)methyl N-phenylcarbamate》 was written by Kavalek, Jaromir; Machacek, Vladimir; Svobodova, Gabriela; Sterba, Vojeslav. Formula: C8H9NO2 And the article was included in Collection of Czechoslovak Chemical Communications on April 30 ,1989. The article conveys some information:

The rate constants of reversible, base-catalyzed ring closure of 3-(methoxycarbonyl)propionanilide (I) and (methoxycarbonylmethyl) phenylcarbamate (II) to 1-phenyl-2,5-pyrrolidinedione (III) and 3-phenyl-2,4-oxazolidinedione (IV), resp., and the rates of solvolyses of III and IV in water and methanol have been determined In both cases, an equilibrium is established between the starting ester and the cyclization product in methoxide solutions, which is strongly shifted in favor of the starting ester. In the case of II in methoxide solutions, the cyclization is followed by a much slower splitting of the cyclization product to give glycolic acid anilide. The effects of X = NH, CH2, O, S in RNHCOXCH2COOMe on the rates of the cyclization and solvolysis of the cyclization products is discussed.2-Hydroxy-N-phenylacetamide(cas: 4746-61-6Formula: C8H9NO2) was used in this study.

2-Hydroxy-N-phenylacetamide(cas: 4746-61-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.Formula: C8H9NO2 The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

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

《Escherichia coli γ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors》 was written by Del Prete, Sonia; Bua, Silvia; Supuran, Claudiu T.; Capasso, Clemente. COA of Formula: C7H9NO2S And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. The article conveys some information:

Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes involved in biosynthetic processes, transport, supply, and balance of CO2/HCO3- into the cell. In Bacteria, CAs avoid the depletion of the dissolved CO2/HCO3- from the cell, providing them to the central metabolism that is compromised without the CA activity. The involvement of CAs in the survival, pathogenicity, and virulence of several bacterial pathogenic species is recent. Here, we report the kinetic properties of the recombinant γ-CA (EcoCAγ) encoded in the genome of Escherichia coli. EcoCAγ is an excellent catalyst for the physiol. CO2 hydration reaction to bicarbonate and protons, with a kcat of 5.7 × 105 s-1 and kcat/Km of 6.9 × 106 M-1s-1. The EcoCAγ inhibition profile with a broad series of known CA inhibitors, the substituted benzene-sulfonamides, and clin. licensed drugs was explored. Benzolamide showed a KI lower than 100 nM. Our study reinforces the hypothesis that the synthesis of new drugs capable of interfering selectively with the bacterial CA activity, avoiding the inhibition of the human α -CAs, is achievable and may lead to novel antibacterials. In the experiment, the researchers used many compounds, for example, 4-Methylbenzenesulfonamide(cas: 70-55-3COA of Formula: C7H9NO2S)

4-Methylbenzenesulfonamide(cas: 70-55-3) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).COA of Formula: C7H9NO2S

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

The author of 《CuCl-catalyzed ortho trifluoromethylation of arenes and heteroarenes with a pivalamido directing group》 were Cai, Shangjun; Chen, Chao; Sun, Zelin; Xi, Chanjuan. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2013. Recommanded Product: 2,2-Dimehtyl-N-pyridin-3-yl-propionamide The author mentioned the following in the article:

The CuCl catalyzed direct trifluoromethylation of sp2 C-H bonds has been realized, using the Togni reagent as the CF3 source. This reaction achieves the goal of regio-selectively converting C-H into C-CF3 with ecol. and readily available starting materials. After reading the article, we found that the author used 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Recommanded Product: 2,2-Dimehtyl-N-pyridin-3-yl-propionamide)

2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Recommanded Product: 2,2-Dimehtyl-N-pyridin-3-yl-propionamide

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

Qin, Zengquan; Jennings, Michael C.; Puddephatt, Richard J. published their research in Chemical Communications (Cambridge, United Kingdom) on December 21 ,2001. The article was titled 《Stacked molecular triangles: self-assembly using coordination chemistry and hydrogen bonding》.HPLC of Formula: 64479-78-3 The article contains the following contents:

The combination of the cis-blocked platinum(II) unit (bu2bipy)Pt2+ with the unsym. bis(pyridine) ligand 4-NC5H4C(:O)NH-4-C5H4N (L) gives the mol. triangle complex [{Pt(bu2bipy)(μ-L)}3]6+, which forms stacked pairs in the solid state through intertriangle NH···OC hydrogen bonds and Pt···OC secondary bonds. The crystal structure of [{(bu2bipy)Pt(μ-L)}3](CF3SO3)6·Me2CO·3H2O was determined The analogous palladium(II) complex was prepared as the BF4- salt.N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3HPLC of Formula: 64479-78-3) was used in this study.

N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors.“,” In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. HPLC of Formula: 64479-78-3

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