M.W=100-150 Archives - Page 7 of 192

Malamas, Michael S.’s team published research in Bioorganic & Medicinal Chemistry Letters in 21 | CAS: 762263-64-9

Bioorganic & Medicinal Chemistry Letters published new progress about 762263-64-9. 762263-64-9 belongs to pyrazines, auxiliary class Pyrazine,Boronic acid and ester,Boronic Acids, name is Pyrazin-2-ylboronic acid, and the molecular formula is C4H5BN2O2, HPLC of Formula: 762263-64-9.

Malamas, Michael S. published the artcileNew pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: Exploring the S2′ region, HPLC of Formula: 762263-64-9, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(18), 5164-5170, database is CAplus and MEDLINE.

The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid in Alzheimer’s disease. SAR studies of the S2′ region of the BACE1 ligand binding pocket with pyrazolyl and thienyl P2′ side chains are reported. These analogs, e.g. I and II, exhibit low nanomolar potency for BACE1, and demonstrate >50- to 100-fold selectivity for the structurally related aspartyl proteases BACE2 and cathepsin D. Small groups attached at the nitrogen of the P2′ pyrazolyl moiety, together with the P3 pyrimidine nucleus projecting into the S3 region of the binding pocket, are critical components to ligand’s potency and selectivity. P2′ thiophene side chain analogs are highly potent BACE1 inhibitors with excellent selectivity against cathepsin D, but only modest selectivity against BACE2. The cell-based activity of these new analogs tracked well with their increased mol. binding with EC₅₀ values of 0.07-0.2 μM in the ELISA assay for the most potent analogs.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Ferguson, Fleur M.’s team published research in Journal of Medicinal Chemistry in 56 | CAS: 4604-72-2

Journal of Medicinal Chemistry published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Computed Properties of 4604-72-2.

Ferguson, Fleur M. published the artcileTargeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain, Computed Properties of 4604-72-2, the publication is Journal of Medicinal Chemistry (2013), 56(24), 10183-10187, database is CAplus and MEDLINE.

Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain using biophys. fragment screening and structure-based optimization of high ligand-efficiency fragments into a novel series of low-micromolar inhibitors. Our results provide attractive leads for development of BAZ2B chem. probes and indicate the whole family may be tractable.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Kaliszan, R.’s team published research in Chromatographia in 10 | CAS: 4604-72-2

Chromatographia published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, SDS of cas: 4604-72-2.

Kaliszan, R. published the artcileThe relationship between the R_M values and the connectivity indexes for pyrazine carbothioamide derivatives, SDS of cas: 4604-72-2, the publication is Chromatographia (1977), 10(7), 346-9, database is CAplus.

An apparent correlation was observed between the R_M values obtained by using reversed-phase thin-layer chromatog. and the mol. connectivity indexes arithmetically computed for various 6-substituted derivatives of 2-pyrazinecarbothioamide. The correlation can be used to identify unknown derivatives

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Kaliszan, Roman’s team published research in Polish Journal of Pharmacology and Pharmacy in 30 | CAS: 4604-72-2

Polish Journal of Pharmacology and Pharmacy published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Synthetic Route of 4604-72-2.

Kaliszan, Roman published the artcileStudies on the quantitative structure-activity relationships in pyrazine carbothioamide derivatives, Synthetic Route of 4604-72-2, the publication is Polish Journal of Pharmacology and Pharmacy (1978), 30(4), 579-83, database is CAplus and MEDLINE.

Quant. structure-activity relations of 1 pyrazinecarbothioamides I (R = NMe₂, SPh, morpholino, etc.) are presented for tuberculostatic potency in vitro. The tuberculostatic activities of I were related both to the size of the substituent and to electronic properties of the mol. An equation [log(1/C) = -0.0221MR + 0.0073λ – 1.6792; MR = molar refractivity calculated for substituents, λ = wave length maximum absorption (nm) C = min. concentration causing inhibition of bacterial growth] was obtained, statistically significant on the 99% level, which described ∼71% of variance of activity data for I as a function of molar refractivity of the substituent and the wave length at which absorption max occurred.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Putta, V. P. Rama Kishore’s team published research in Organic & Biomolecular Chemistry in 17 | CAS: 4604-72-2

Organic & Biomolecular Chemistry published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Recommanded Product: Pyrazine-2-carbothioamide.

Putta, V. P. Rama Kishore published the artcileA metal- and base-free domino protocol for the synthesis of 1,3-benzoselenazines, 1,3-benzothiazines and related scaffolds, Recommanded Product: Pyrazine-2-carbothioamide, the publication is Organic & Biomolecular Chemistry (2019), 17(9), 2516-2528, database is CAplus and MEDLINE.

Efficient protocols have been described for the synthesis of 1,3-benzoselenazines, 1,3-benzothiazines, 2-arylthiazin-4-ones and diaryl[b,f][1,5]diazocine-6,12(5H,11H)-diones. These transformations were successfully driven towards product formation under mild acid catalyzed reaction conditions at room temperature using 2-aminoaryl/hetero-aryl alkyl alcs. and amides as substrates. The merits of the present methods also rely on the easy access of rarely explored bioactive scaffolds like 1,3-benzoselenazine derivatives, for which well-documented methods are rarely known in the literature. A broad range of substrates with both electron-rich and electron-deficient groups were well-tolerated under the developed conditions to furnish the desired products in yields up to 98%. The scope of the devised method was not only restricted to the synthesis of 1,3-benzoselenazines, but it was further extended towards the synthesis of 1,3-benzothiazines, 1,3-benzothiazinones and the corresponding eight-membered N-heterocycles such as diaryl[b,f][1,5]diazocine-6,12(5H,11H)-diones.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Wang, Zhuolin’s team published research in Journal of Agricultural and Food Chemistry in 2020-01-08 | CAS: 14667-55-1

Journal of Agricultural and Food Chemistry published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Related Products of pyrazines.

Wang, Zhuolin published the artcileCharacterization of aroma-active compounds in four yeast extracts using instrumental and sensory techniques, Related Products of pyrazines, the main research area is aroma yeast extract olfactometry GC; aroma-active compounds; gas chromatography−olfactometry; odor activity value; partial least-squares regression; solvent-assisted flavor evaporation; yeast extracts.

Gas chromatog.-olfactometry coupled with sensory anal. and partial least-squares regression (PLSR) anal. led to the identification of the odorants responsible for the different flavors of four yeast extracts Sensory anal. showed that LA00L had an intense sulfurous attribute, and LA00 was characterized by fatty and green notes, FA31 exhibited the floral odor, while KA02 had strong phenolic, animal, fermented, roasted, and caramellic notes. A total of 37 key aroma compounds with odor activity values greater than 1 were determined 2,4-Di-tert-butylphenol and methional were the most potent aroma compounds In addition, the key aroma compounds in LA00L were nonanal, di-Me disulfide, and γ-decalactone. Octanal, di-Me disulfide, and benzeneacetaldehyde were the key aroma compounds in LA00. In FA31, styrene, benzeneacetaldehyde, and acetophenone were the key aroma compounds, while indole, 2-methoxyphenol, benzeneacetaldehyde, and p-cresol contributed significantly to the aroma of KA02. PLSR showed that p-cresol and indole were significantly responsible for the phenolic and animal notes inducing the off-flavor (yeasty odor) of yeasty extracts More significantly, indole was first reported to have an important effect on yeasty odor.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ling, Hongzhi’s team published research in Food Chemistry in 2022-04-16 | CAS: 14667-55-1

Food Chemistry published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Formula: C7H10N2.

Ling, Hongzhi published the artcileDetection of the microbial diversity and flavour components of northeastern Chinese soybean paste during storage, Formula: C7H10N2, the main research area is Firmicutes Actinobacteriota soybean paste storage flavor volatile component; Flavour Components; GC-IMS; Microbial community; Soybean paste.

A combination of 16S rDNA and GC-IMS was used to study the changes in the composition of microorganisms and volatile organic compounds (VOCs) during the storage of northeastern Chinese soybean paste. Firmicutes and Actinobacteriota dominated the microbial communities of the soybean paste at the phylum level, bacterial profiles of different samples were different at genus level. Fifty-one VOCs were identified from soybean paste, most of which existed in the early storage stage. Most esters and alcs. decreased with the extension of the storage time, while acids and pyrazines accumulated in the later period of storage. Esters, alcs., acids and aldehyde compounds are the key substances in the volatile components of soybean paste, which give the soybean paste the sour, sweet, rose, mushroom and smoky flavor characteristics. The biomarker Bacillus-velezensis in soybean paste is directly related to ester features; Kroppenstedtia, Sporolactobacillus-nakayamae, and Corynebacterium-stationis are pos. associated with the biosynthesis of aldehydes.

Food Chemistry published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Formula: C7H10N2.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Zhang, Yukun’s team published research in Journal of Cereal Science in 2020-05-31 | CAS: 14667-55-1

Journal of Cereal Science published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Synthetic Route of 14667-55-1.

Zhang, Yukun published the artcileCharacterization and comparison of predominant aroma compounds in microwave-treated wheat germ and evaluation of microwave radiation on stability, Synthetic Route of 14667-55-1, the main research area is wheat germ lipase lipoxygenase aroma flavor color microwave radiation.

The present study was performed to evaluate the effects of microwave (MW) output power and treatment time on moisture content, lipase and lipoxygenase activities as well as color changes of wheat germ (WG). In addition, the key aroma compounds in different MW-power-treated WG, which is of importance to the flavor of WG products, were also investigated. The obtained results showed that MW treatment maintained the inherent color of WG and significantly reduced the moisture content (maximum reduction of 95%) and the activities of lipase and lipoxygenase (maximum reduction of 65% and 99%, resp.). In terms of aroma compounds, with the increase of the MW output power, the content of esters, alkanes, alcs. and acids decreased, while the content of heterocyclic compounds, nitrogen-containing compounds, aldehydes and ketones increased, providing more compounds with roasted flavor and less volatiles with grass-like flavor. Therefore, MW treatment was an effective stabilization method for WG utilization.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Guo, Xiangyang’s team published research in Food Chemistry in 2021-06-15 | CAS: 14667-55-1

Food Chemistry published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Safety of 2,3,5-Trimethylpyrazine.

Guo, Xiangyang published the artcileEffect of the roasting degree on flavor quality of large-leaf yellow tea, Safety of 2,3,5-Trimethylpyrazine, the main research area is catechin caffeine large leaf yellow tea roasting flavor quality; Flavor quality; Heterocyclic compounds; Large-leaf yellow tea (LYT); Odor activity values (OAV); Roasting degree; Sensory evaluation.

Roasting is crucial for producing large-leaf yellow tea (LYT) as it substantially affects chem. composition and sensory quality. However, the effect of roasting degree on LYT flavor quality is not clear. To investigate the effect of roasting degree on LYT flavor, the odor profiles and sensory evaluations of LYTs produced with small fire, medium fire and old fire roasting (OF) were determined The OF was essential for the formation of LYT flavor with strong roasted, nutty, woody odors and weak fatty, fruity odors, and retaining high levels of GCG, total volatiles and heterocyclic compounds Furthermore, the characteristic crispy-rice-like odor was only found in LYT with OF treatment and burnt flavor was missing. 2,3-Diethyl-5-methylpyrazine, trans-β-ionone with odor activity value above 1600 and 39 resp. offered roasted, floral odors, resp. in LYT. The current results provide a scientific basis for understanding the reactions that occur during the conventional production of LYT.

Food Chemistry published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Safety of 2,3,5-Trimethylpyrazine.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Jelen, Henryk H.’s team published research in LWT–Food Science and Technology in 2019-06-30 | CAS: 14667-55-1

LWT–Food Science and Technology published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Formula: C7H10N2.

Jelen, Henryk H. published the artcileKey odorants in peated malt whisky and its differentiation from other whisky types using profiling of flavor and volatile compounds, Formula: C7H10N2, the main research area is peated malt whisky odorant flavor volatile compound.

Key odorants of peated single malt whisky were identified using gas chromatog. – olfactometry (GC-O). Twenty compounds were identified with FD (Flavor Dilution) values ranging from 8 to 2048 and 8 of them were volatile phenols. The compounds with the highest FD were 2-methoxyphenol (guaiacol), 4-ethyl-2-methoxyphenol (4-ethylguaiacol), 4-methylphenol, 4-vinyl-2-methoxyphenol (4-vinylguaiacol) and 4-ethyl-2-methylphenol (FD ranging from 512 to 2048). Then odorants were used successfully to distinguish peated single malts from 3 other whisky types (mild single malts, blended and American whiskies) based on PCA followed by LDA applied to GC×GC-ToF MS data of volatiles extracted using SPME. 36 Whiskies representing all groups were used for the differentiation experiments Finally, 61 volatile compounds based on Fisher ratios were selected to fully discriminate between 4 whisky types based on profile of volatiles obtained in SPME-GC×GC-ToF MS anal. Cross-validation confirmed the suitability of PCA and LDA models for the discrimination of different whisky types.

LWT–Food Science and Technology published new progress about Flavor. 14667-55-1 belongs to class pyrazines, name is 2,3,5-Trimethylpyrazine, and the molecular formula is C7H10N2, Formula: C7H10N2.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem