Month: October 2022

Bakhache, William’s team published research in Antiviral Research in 2019-12-31 | 96829-58-2

Antiviral Research published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

Bakhache, William; Neyret, Aymeric; McKellar, Joe; Clop, Camille; Bernard, Eric; Weger-Lucarelli, James; Briant, Laurence published the artcile< Fatty acid synthase and stearoyl-CoA desaturase-1 are conserved druggable cofactors of Old World Alphavirus genome replication>, SDS of cas: 96829-58-2, the main research area is Chikungunya virus; Fatty acid synthase; Genome replication; Lipid metabolism; Mayaro virus; Stearoyl-CoA desaturase-1.

Chikungunya virus (CHIKV) is a rapidly emerging mosquito-borne RNA virus that causes epidemics of debilitating disease in tropical and sub-tropical regions with autochtonous transmission in regions with temperate climate. Currently, there is no licensed vaccine or specific antiviral drug available against CHIKV infection. In this study, we examine the role, in the CHIKV viral cycle, of fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD1), two key lipogenic enzymes required for fatty acid production and early desaturation We show that both enzymes and their upstream regulator PI3K are required for optimal CHIKV infection. We demonstrate that pharmacol. manipulation of FASN or SCD1 enzymic activity by non-toxic concentrations of cerulenin or CAY10566 decreases CHIKV genome replication. Interestingly, a similar inhibitory effect was also obtained with Orlistat, an FDA-approved anti-obesity drug that targets FASN activity. These drugs were also effective against Mayaro virus (MAYV), an under-studied arthritogenic Old world Alphavirus endemic in South American countries with potential risk of emergence, urbanization and dispersion to other regions. Altogether, our results identify FASN and SCD1 as conserved druggable cofactors of Alphavirus genome replication and support the broad-spectrum activity of drugs targeting the host fatty acids metabolism

Antiviral Research published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

Karatas, Mehmet’s team published research in Molecules in 2021 | 25999-04-6

Molecules published new progress about Antiproliferative agents. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Related Products of 25999-04-6.

Karatas, Mehmet; Chaikuad, Apirat; Berger, Bianca; Kubbutat, Michael H. G.; Totzke, Frank; Knapp, Stefan; Kunick, Conrad published the artcile< 7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones designed by a ""cut and glue"" strategy are dual Aurora A/VEGF-R kinase inhibitors>, Related Products of 25999-04-6, the main research area is anilinopyrimidinyl benzazepinone AuroraA VEGFR kinase inhibitor; Aurora kinase; X-ray structure analysis; anilinopyrimidine; benzazepinone; molecular docking; protein kinase inhibitor; sulfamide.

Although overexpression and hyperactivity of protein kinases are causative for a wide range of human cancers, protein kinase inhibitors currently approved as cancer drugs address only a limited number of these enzymes. To identify new chemotypes addressing alternative protein kinases, the basic structure of a known PLK1/VEGF-R2 inhibitor class was formally dissected and reassembled. The resulting 7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones were synthesized and proved to be dual inhibitors of Aurora A kinase and VEGF receptor kinases. Crystal structures of two representatives of the new chemotype in complex with Aurora A showed the ligand orientation in the ATP binding pocket and provided the basis for rational structural modifications. Congeners with attached sulfamide substituents retained Aurora A inhibitory activity. In vitro screening of two members of the new kinase inhibitor family against the cancer cell line panel of the National Cancer Institute (NCI) showed antiproliferative activity in the single-digit micromolar concentration range in the majority of the cell lines.

Molecules published new progress about Antiproliferative agents. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Related Products of 25999-04-6.

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

Sivaramakrishna, Mallampalli’s team published research in Separation and Purification Technology in 2017-06-30 | 5326-82-9

Separation and Purification Technology published new progress about Extraction. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Product Details of C10H20ClNO.

Sivaramakrishna, Mallampalli; Raut, Dhaval R.; Nayak, Shashikant; Nayak, Sandip K.; Mohapatra, Prasanta K. published the artcile< Unusual selective extraction of Pu4+ by some novel diamide ligands in a room temperature ionic liquid>, Product Details of C10H20ClNO, the main research area is plutonium selective extraction diamide ligand ionic liquid uranyl ion.

Extraction of Pu4+ was carried out from nitric acid feeds employing ionic liquid solutions of four novel diamide ligands containing an aromatic bridging group. The ligands with iso-Bu, Bu, n-octyl and 2-ethylhexyl groups were termed as LI, LII, LIII, and LIV, resp. and showed significantly higher extraction of the tetravalent plutonium ion as compared to the hexavalent uranyl ion. Using 0.05 M ligands, the extraction of Pu4+ was in the range of 80-95% when 3 M HNO3 was used as the feed and followed the order: LIII > LII > LI > LIV while the UO22+ ion extraction was less than 4-5% and no particular trend could be established. The extraction of UO22+ could be partly due to the anionic nitrate complex of uranyl ion which was extracted in the absence of the ligands, while the ligand assisted extraction contributing for the remaining. Out of the other metal ions studied, Cs+ showed some extraction which was not ligand assisted while almost no extraction of metal ions such as Sr2+, Am3+ and Eu3+ was noticed. Unusually high selectivity was seen for Pu4+ ion extraction out of all the metal ions studied making the solvent systems very important for a plutonium specific separation method development. The extraction was found to be increasing with the aqueous phase nitric acid concentration conforming to a ‘solvation mechanism’ of extraction where the extracted species conforming to Pu(NO3)4·LIL for all the four diamide extractants.

Separation and Purification Technology published new progress about Extraction. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Product Details of C10H20ClNO.

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

El-Shal, Laila Moustafa’s team published research in Ultrastructural Pathology in 2022 | 96829-58-2

Ultrastructural Pathology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

El-Shal, Laila Moustafa; El-Star, Alyaa A. Abd; Azmy, Abeer M.; Elnegris, Heba M. published the artcile< The possible protective role of N-acetyl cysteine on duodenal mucosa of high fat diet and orlistat treated adult male albino rats and the active role of tumor necrosis factor α (TNFα) and Interleukin 6 (IL6) (histological and biochemical study)>, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is HFD; IL6; N-acetyl cysteine; Orlistat; TNFα; duodenal mucosa.

BackgroundObesity is a major universal health issue linked to a majority of illness. AimTo evaluate the histol. and biochem. changes occurred in the duodenal mucosa of high fat diet HFD and orlistat fed rats and to assess the possible protective role of N-acetyl cysteine NAC supplementation. Material and methodSixty male albino rats weighing 180-200 g were classified randomly into control group I and three exptl. groups (HFD group II, HFD + orlistat group III, and HFD + orlistat + NAC group IV). All exptl. groups received HFD alone/and treatment for 6 wk. Group III received orlistat (32 mg/kg/day) before meals and group IV received the same regimen as group III in addition to NAC (230 mg/kg/day) after meals. After completion of the experiment, duodenal sections were processed for histol. examination, oxidative stress parameters, and semiqualitative real time PCR for proinflammatory mediators TNFα and IL6 evaluation. Also, plasma lipid parameters were assessed and morphometric duodenal results were analyzed statistically. ResultsBy histol. examination of HFD and (HFD + orlistat) groups, we found severe to moderate duodenal structural disturbances, increased goblet cells, collagen fibers, and BAX and iNOS immunostaining. By Biochem. examination, both groups showed increased proinflammatory markers level (TNFα and IL6) with decreased all antioxidant parameters and increased MDA. Moreover, NAC treatment in group IV significantly reduced all structural changes, levels of proinflammatory mediators and increased all antioxidant parameter levels and decreased MDA. ConclusionAll findings elucidated that NAC could be accounted to be a useful drug for protection of duodenal mucosa of HFD and orlistat treated animals.

Ultrastructural Pathology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Huffman, Tucker R.’s team published research in Angewandte Chemie, International Edition in 2019 | CAS: 71432-55-8

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Quality Control of tert-Butyl N,N’-diisopropylcarbamimidate

Quality Control of tert-Butyl N,N’-diisopropylcarbamimidateIn 2019 ,《Intermolecular Heck Coupling with Hindered Alkenes Directed by Potassium Carboxylates》 appeared in Angewandte Chemie, International Edition. The author of the article were Huffman, Tucker R.; Wu, Yebin; Emmerich, Alexis; Shenvi, Ryan A.. The article conveys some information:

Pd0-catalyzed Mizoroki-Heck reactions traditionally exhibit poor reactivity with polysubstituted, unbiased alkenes. Intermol. reactions with simple, all-carbon tetrasubstituted alkenes are unprecedented. Herein we report that pendant carboxylic acids, combined with bulky monophospine ligands on palladium, can direct the arylation of tri- and tetrasubstituted olefins. Quaternary carbons are established at high Fsp3 attached-ring junctures and the carboxylate directing group can be removed after coupling. Carboxylate directivity prevents over-arylation of the new, less substituted alkene, which can be diversified in subsequent reactions. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Quality Control of tert-Butyl N,N’-diisopropylcarbamimidate)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Quality Control of tert-Butyl N,N’-diisopropylcarbamimidate

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

Buil, Maria Antonia’s team published research in European Journal of Medicinal Chemistry in 2016 | CAS: 78191-00-1

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Safety of N-Methoxy-N-methylacetamide

Safety of N-Methoxy-N-methylacetamideIn 2016 ,《Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists》 was published in European Journal of Medicinal Chemistry. The article was written by Buil, Maria Antonia; Calbet, Marta; Castillo, Marcos; Castro, Jordi; Esteve, Cristina; Ferrer, Manel; Forns, Pilar; Gonzalez, Jacob; Lopez, Sara; Roberts, Richard S.; Sevilla, Sara; Vidal, Bernat; Vidal, Laura; Vilaseca, Pere. The article contains the following contents:

Monocyclic and bicyclic ring systems were studied as the “”core”” section of a series of diphenylsulfone-containing acetic acid CRTh2 receptor antagonists. A range of potencies were observed and single-digit nanomolar potencies were obtained in both the monocyclic and bicyclic cores. Residence times for the monocyclic compounds were very short. Some of the bicyclic cores displayed better residence times. A Me group in the northern part of the core, between the head and tail was a necessary requirement for the beginnings of long residence times. Variations of the tail substitution maximized potencies and residence times. The experimental part of the paper was very detailed, including the reaction process of N-Methoxy-N-methylacetamide(cas: 78191-00-1Safety of N-Methoxy-N-methylacetamide)

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Safety of N-Methoxy-N-methylacetamide

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

Kawamata, Takahiro’s team published research in Journal of the American Chemical Society in 2017 | CAS: 71432-55-8

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.HPLC of Formula: 71432-55-8

《Total Synthesis of Zaragozic Acid C: Implementation of Photochemical C(sp3)-H Acylation》 was written by Kawamata, Takahiro; Nagatomo, Masanori; Inoue, Masayuki. HPLC of Formula: 71432-55-8This research focused onzaragozic acid photochem acylation synthesis Norrish Yang cyclization hydroxycyclobutanone. The article conveys some information:

Zaragozic acid C was isolated as a potent squalene synthase inhibitor. The 2,8-dioxabicyclo[3.2.1]octane core of 1 is decorated with the three hydroxycarbonyl (C3,4,5), two hydroxy (C4,7), one acyloxy (C6), and one alkyl (C1) groups. Installation of the contiguous C4- and C5-fully substituted carbons presents a formidable synthetic challenge. Our approach to address this problem used a two-step photochem. C(sp3)-H acylation. Persilylated D-gluconolactone was derivatized with the 1,2-diketone moiety at the C5-tetra-substituted center. Norrish-Yang cyclization of 3 under violet LED irradiation followed by oxidative opening of the resultant α-hydroxycyclobutanone regio- and stereoselectively transformed the electron-rich tertiary C(sp3)-H bond at C4 into a C(sp3)-C bond. A subsequent series of judicious functional group transformations gave rise to zaragozic acid C. In addition to this study using tert-Butyl N,N’-diisopropylcarbamimidate, there are many other studies that have used tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8HPLC of Formula: 71432-55-8) was used in this study.

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.HPLC of Formula: 71432-55-8

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

Abdelkader, Elwy H.’s team published research in Journal of the American Chemical Society in 2021 | CAS: 2418-95-3

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. These amino acids may be present in low concentrations and play a vital part as an intermediate in a biosynthetic pathway, e.g., ornithine, homoserine, or cystathionine. In contrast they may act as a major storage form of nitrogen, e.g., canavanine in the seed of Canavalia ensiformis, or may be formed in high amounts in response to an external stress, e.g., γ-aminobutyrate.Computed Properties of C11H22N2O4 It is possible that some of these nonprotein amino acids may serve as insecticidal or fungicidal agents.

Abdelkader, Elwy H.; Qianzhu, Haocheng; Tan, Yi Jiun; Adams, Luke A.; Huber, Thomas; Otting, Gottfried published an article on January 20 ,2021. The article was titled 《Genetic Encoding of N6-(((Trimethylsilyl)methoxy)carbonyl)-L-lysine for NMR Studies of Protein-Protein and Protein-Ligand Interactions》, and you may find the article in Journal of the American Chemical Society.Computed Properties of C11H22N2O4 The information in the text is summarized as follows:

Trimethylsilyl (TMS) groups present outstanding NMR probes of biol. macromols. as they produce intense singlets in 1H NMR spectra near 0 ppm, where few other proton resonances occur. We report a system for genetic encoding of N6-(((trimethylsilyl)methoxy)carbonyl)-L-lysine (TMSK) for site-specific incorporation into proteins. The system is based on pyrrolysyl-tRNA synthetase mutants, which deliver proteins with high yield and purity in vivo and in cell-free protein synthesis. As the TMS signal can readily be identified in 1D 1H NMR spectra of high-mol. weight systems without the need of isotopic labeling, TMSK delivers an excellent site-specific NMR probe for the study of protein structure and function, which is both inexpensive and convenient. We demonstrate the utility of TMSK to detect ligand binding, measure the rate of conformational change, and assess protein dimerization by paramagnetic relaxation enhancement. In addition, we present a system for dual incorporation of two different unnatural amino acids (TMSK and O-tert-butyl-tyrosine) in the same protein in quantities sufficient for NMR spectroscopy. Close proximity of the TMS and tert-Bu groups was readily detected by nuclear Overhauser effects. The experimental part of the paper was very detailed, including the reaction process of H-Lys(Boc)-OH(cas: 2418-95-3Computed Properties of C11H22N2O4)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. These amino acids may be present in low concentrations and play a vital part as an intermediate in a biosynthetic pathway, e.g., ornithine, homoserine, or cystathionine. In contrast they may act as a major storage form of nitrogen, e.g., canavanine in the seed of Canavalia ensiformis, or may be formed in high amounts in response to an external stress, e.g., γ-aminobutyrate.Computed Properties of C11H22N2O4 It is possible that some of these nonprotein amino acids may serve as insecticidal or fungicidal agents.

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

Andres, J. Ignacio’s team published research in Bioorganic & Medicinal Chemistry Letters in 2002 | CAS: 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.Application of 70298-88-3

Andres, J. Ignacio; Alonso, Jose M.; Fernandez, Javier; Iturrino, Laura; Martinez, Pedro; Meert, Theo F.; Sipido, Victor K. published their research in Bioorganic & Medicinal Chemistry Letters on December 16 ,2002. The article was titled 《2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT2C antagonist with potential anxiolytic properties》.Application of 70298-88-3 The article contains the following contents:

The synthesis of 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,4-c]-[2]benzazepine and 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,2-c]-[2]benzazepine via a new route is reported. The affinities for several receptors as well as the m-chlorophenylpiperazine antagonistic activity of the compounds synthesized are described. After reading the article, we found that the author used 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Application 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.Application of 70298-88-3

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

Robertson, Wesley E.’s team published research in Science (Washington, DC, United States) in 2021 | CAS: 2418-95-3

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).Application of 2418-95-3

The author of 《Sense codon reassignment enables viral resistance and encoded polymer synthesis》 were Robertson, Wesley E.; Funke, Louise F. H.; de la Torre, Daniel; Fredens, Julius; Elliott, Thomas S.; Spinck, Martin; Christova, Yonka; Cervettini, Daniele; Boge, Franz L.; Liu, Kim C.; Buse, Salvador; Maslen, Sarah; Salmond, George P. C.; Chin, Jason W.. And the article was published in Science (Washington, DC, United States) in 2021. Application of 2418-95-3 The author mentioned the following in the article:

It is widely hypothesized that removing cellular tRNAs (tRNAs)-making their cognate codons unreadable-might create a genetic firewall to viral infection and enable sense codon reassignment. However, it has been impossible to test these hypotheses. In this work, following synonymous codon compression and laboratory evolution in Escherichia coli, we deleted the tRNAs and release factor 1, which normally decode two sense codons and a stop codon; the resulting cells could not read the canonical genetic code and were completely resistant to a cocktail of viruses. We reassigned these codons to enable the efficient synthesis of proteins containing three distinct noncanonical amino acids. Notably, we demonstrate the facile reprogramming of our cells for the encoded translation of diverse noncanonical heteropolymers and macrocycles. In the experiment, the researchers used H-Lys(Boc)-OH(cas: 2418-95-3Application of 2418-95-3)

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).Application of 2418-95-3

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