Month: November 2022

Adamova, Katerina published the artcileAntifungal action of acylated thioamides and related compounds, Name: Pyrazine-2-carbothioamide, the publication is Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium (1991), 102(Chem. 30), 155-60, database is CAplus.

Some acylated thioamides and similar compounds were tested for their antifungal properties. Only 3 thioamides, thiophthalic anhydride, and some thiuram disulfides had good activity. The condensation of thioamides with Me isothiocyanate gave active compounds The activity of thiuram disulfides was related to the solubility in water.

Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium 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, Name: Pyrazine-2-carbothioamide.

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

Lumma, William C. Jr. published the artcilePiperazinylpyrazines with central serotoninmimetic activity, Application of 2-Chloro-6-(trifluoromethyl)pyrazine, the publication is Journal of Medicinal Chemistry (1978), 21(6), 536-42, database is CAplus and MEDLINE.

Twenty title compounds I [R = H, [CH₂)₃NMe₂, or 6-chloro-2-pyrazinyl; R = H or Cl; R² = H, Cl, Ph, or CO₂Me; R³ = H, Cl, Me, SPh, etc.; X = 2H or O] were synthesized by reaction of the appropriate chloropyrazine with piperazine [110-85-0] or an N-substituted piperazine. I; (R = R¹ = R² = H; R³ = Cl; X = 2H,.HCl) [61655-58-1] had pharmacol. properties in mice characteristic of potent central serotoninmimetic activity and only weak peripheral serotoninmimetic action in isolated rat uterus. Preferred conformations of this compound, determined by classical strain energy calculations and CNDO mol. orbital techniques, were compared with serotonin [50-67-9] in order to determination those structural features which might interact with serotonin receptors.

Journal of Medicinal Chemistry published new progress about 61655-69-4. 61655-69-4 belongs to pyrazines, auxiliary class Trifluoromethyl,Pyrazine,Fluoride,Chloride, name is 2-Chloro-6-(trifluoromethyl)pyrazine, and the molecular formula is C5H2ClF3N2, Application of 2-Chloro-6-(trifluoromethyl)pyrazine.

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

Rada, B. published the artcileInhibition of virus multiplication by some derivatives of pyridine- and pyrazinecarboxylic acid, Recommanded Product: Pyrazine-2-carbothioamide, the publication is Acta Virologica (English Edition) (1971), 15(4), 326-8, database is CAplus and MEDLINE.

In agar-diffusion plaque-inhibition test with 25 derivatives of pyridine- and pyrazinemono-carboxylic acid, 2-bromo-4-thiocarbamoylpyridine (I) was found effective against vaccinia virus, forming an inhibition zone of medium size without any toxic effect, while 2,6-diethoxy-4-hydroxycarbamoylpyridine and 2-butoxy-4-hydroxycarbamoylpyridine formed large zones of inhibition against vaccinia and western equine encephalomyelitis viruses together with smaller toxic zones.

Acta Virologica (English Edition) 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.

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

Wang, Changliu published the artcileYnamide-Mediated Thioamide and Primary Thioamide Syntheses, Name: Pyrazine-2-carbothioamide, the publication is Journal of Organic Chemistry (2022), 87(9), 5617-5629, database is CAplus and MEDLINE.

Environmentally friendly ynamide-mediated thioamidation of monothiocarboxylic acids with amines or ammonium hydroxide for the synthesis of thioamides was described. Simple and mild reaction conditions tolerate a wide variety of functional groups such as hydroxyl, ester, tertiary amine, ketone, and amide moieties. Readily available NaSH served as the sulfur source, avoiding the use of toxic, expensive, and malodorous organic sulfur reagents and making this strategy environmentally friendly and practical. Importantly, the stereochem. integrity of α-chiral monothiocarboxylic acids was maintained during the activation step and subsequent aminolysis process, which offers a racemization-free strategy for peptide and protein C-terminal modification. Furthermore, a number of thioamide-modified drugs were prepared in good yields by this protocol and the synthesized primary thioamides were transformed into backbone thiazolyl modification peptides.

Journal of Organic 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 C6H8O3, Name: Pyrazine-2-carbothioamide.

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

Gampe, Dominique Mario published the artcileMixing Chromophores: Donor-Acceptor Dyes with Low-Lying LUMOs and Narrow Band Gaps by Connecting 4-Alkoxythiazoles and Azaacenes, Related Products of pyrazines, the publication is European Journal of Organic Chemistry (2017), 2017(10), 1369-1379, database is CAplus.

The synthesis and characterization of novel donor-acceptor (D-A) type functional dyes is presented. The materials studied are based on the 4-alkoxythiazole structure containing one of three arylamine donor units and one of three acceptor building blocks. The nine dyes were characterized with respect to their photo- and electrochem. properties based on UV/Vis absorption and fluorescence emission spectroscopy, and cyclic voltammetry. D. functional theory calculations were carried out to support these studies. The building blocks used brought their characteristics into the final target structures: the reversible oxidation and electron-donating properties of diarylamines, the high fluorescence quantum yields of 4-alkoxythiazoles, and the low-lying LUMOs of tetraazaanthracenes. Furthermore, by introducing tetraazaanthracenes as the acceptor moiety, narrow band gaps of 1.1 and 0.7 eV were estimated electrochem.

European Journal of Organic 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, Related Products of pyrazines.

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

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.

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.

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

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.

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.

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

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

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.

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

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.

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.

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

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.

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.

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