Month: April 2022

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor, the main research direction is neuropathic pain safety GSH preclin CYP3A4 sodium channels inhibitor.SDS of cas: 591-54-8.

A highly potent, selective NaV1.7 inhibitor, DS-1971a(I), has been discovered. Exploration of the left-hand Ph ring of sulfonamide derivatives (I and II) led to the discovery of novel series of cycloalkane derivatives with high NaV1.7 inhibitory potency in vitro. As the right-hand heteroaromatic ring affected the mechanism-based inhibition liability of CYP3A4, replacement of this moiety resulted in the generation of 4-pyrimidyl derivatives Addnl., GSH adducts formation, which can cause idiosyncratic drug toxicity, was successfully avoided by this modification. An addnl. optimization led to the discovery of DS-1971a. In preclin. studies, DS-1971a demonstrated highly potent selective in vitro profile with robust efficacy in vivo. DS-1971a exhibited a favorable toxicol. profile, which enabled multiple-dose studies of up to 600 mg bid or 400 mg tid (1200 mg/day) administered for 14 days to healthy human males. DS-1971a is expected to exert potent efficacy in patients with peripheral neuropathic pain, with a favorable safety profile.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Video-Audio Media, Journal of Visualized Experiments called Generation and on-demand initiation of acute ictal activity in rodent and human tissue, Author is Chang, Michael; Dufour, Suzie; Carlen, Peter L.; Valiante, Taufik A., which mentions a compound: 591-54-8, SMILESS is C1=CN=CN=C1N, Molecular C4H5N3, Category: pyrazines.

Controlling seizures remains a challenging issue for the medical community. To make progress, researchers need a way to extensively study seizure dynamics and investigate its underlying mechanisms. Acute seizure models are convenient, offer the ability to perform electrophysiol. recordings, and can generate a large volume of electrog. seizure-like (ictal) events. The promising findings from acute seizure models can then be advanced to chronic epilepsy models and clin. trials. Thus, studying seizures in acute models that faithfully replicate the electrog. and dynamical signatures of a clin. seizure will be essential for making clin. relevant findings. Studying ictal events in acute seizure models prepared from human tissue is also important for making findings that are clin. relevant. The key focus in this paper is on the cortical 4-AP model due to its versatility in generating ictal events in both in vivo and in vitro studies, as well as in both mouse and human tissue. The methods in this paper will also describe an alternative method of seizure induction using the Zero-Mg2+ model and provide a detailed overview of the advantages and limitations of the epileptiform-like activity generated in the different acute seizure models. Moreover, by taking advantage of com. available optogenetic mouse strains, a brief (30 ms) light pulse can be used to trigger an ictal event identical to those occurring spontaneously. Similarly, 30 – 100 ms puffs of neurotransmitters (Gamma-Amino Butyric Acid or glutamate) can be applied to the human tissue to trigger ictal events that are identical to those occurring spontaneously. The ability to trigger ictal events on-demand in acute seizure models offers the newfound ability to observe the exact sequence of events that underlie seizure initiation dynamics and efficiently evaluate potential anti-seizure therapies.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Application of 118994-89-1. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Copper-catalyzed diarylation of Se with aryl iodides and heterocycles. Author is Hu, Dehua; Liu, Miaochang; Wu, Huayue; Gao, Wenxia; Wu, Ge.

The regioselective copper-catalyzed three-component coupling reaction of electron-deficient heterocycles, like aryl-oxadiazoles/aryloxazoles/dimethyl-purine-diones, etc. with aryl iodides in presence of Se powder so as to yield corresponding diaryl-selenated heterocycles such as arylselanyl-aryl-oxadiazoles I [R = Ph, 4-MeC6H4, 2-thienyl, etc.; R1 = Ph, 2-naphthyl, 3-thienyl, etc.] and arylselanyl-aryl-oxazoles II [R2 = Ph, 2,4,6-triMeC6H2; R3 = CO2Et, Ph, 4-MeSC6H4, etc.] was disclosed. The established methodol. provided an efficient and practical pathway to access arylselenated heterocycles via copper-catalyzed double C-Se bond formation. This transformation featured the use of elemental Se as the selenating reagent, a cost-effective catalytic system and the late-stage selenation of bioactive compounds

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Category: pyrazines. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about The stability of L-ATC hydrolase participating in L-cysteine production.

In the production of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC), the stability of the relevant enzymes produced by Pseudomonas sp. was tested, and strategies to improve the stability of L-ATC hydrolase were investigated with respect to water activity and ionic strength. Among the 3 enzymes which participate in L-cysteine production, i.e., ATC racemase, L-ATC hydrolase, and S-carbamyl-L-cysteine hydrolase, L-ATC hydrolase is the least stable. Various mixtures of salts and sorbitol were added to adjust the water activities of the tested solutions As the water activity decreased from 0.93 to 0.80, the stability of L-ATC hydrolase was sharply enhanced. In the absence of sorbitol, the stability of L-ATC hydrolase increased in proportion to ionic strength. Even though enzyme stability was not good at a low ionic strength, it was enhanced by lowering the water activity with the addition of sorbitol. The half-life of L-ATC hydrolase in sorbitol-salt mixtures increased by 10- to 20-fold compared to that of a control.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Novel pyrazolopyrimidines as highly potent B-Raf inhibitors》. Authors are Di Grandi, Martin J.; Berger, Dan M.; Hopper, Darrin W.; Zhang, Chunchun; Dutia, Minu; Dunnick, Alejandro L.; Torres, Nancy; Levin, Jeremy I.; Diamantidis, George; Zapf, Christoph W.; Bloom, Jonathan D.; Hu, YongBo; Powell, Dennis; Wojciechowicz, Donald; Collins, Karen; Frommer, Eileen.The article about the compound:3-(Pyridin-4-yl)-1H-pyrazol-5-aminecas:91912-53-7,SMILESS:NC1=CC(C2=CC=NC=C2)=NN1).Product Details of 91912-53-7. Through the article, more information about this compound (cas:91912-53-7) is conveyed.

A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a replacement for the C(3) phenol demonstrated indazole to be an effective isostere. Several compounds possessing substituted indazole residues, such as 4e, 4p, and 4r, potently inhibited cell proliferation at submicromolar concentrations in the A375 and WM266 cell lines, and the latter two compounds also exhibited good therapeutic indexes in cells.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Huai, Lihua; Chen, Ning researched the compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2 ).Name: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.They published the article 《Effect of dissolved oxygen on production of L-cysteine synthetase by Pseudomonas sp. TS1138》 about this compound( cas:2150-55-2 ) in Shipin Kexue (Beijing, China). Keywords: dissolved oxygen cysteine synthetase Pseudomonas fermentation. We’ll tell you more about this compound (cas:2150-55-2).

Pseudomonas sp. TS1138 has potential to produce L-cysteine synthetase through asym. hydrolysis of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC). The effect of dissolved oxygen level on the production of L-cysteine synthetase was investigated in shake flasks or 7 L bioreactor. The results indicated that the cell growth and the production of L-cysteine synthetase were inhibited at low dissolved oxygen level. Although cell growth was improved at the high dissolved oxygen level, the inhibition against production of L-cysteine synthetase was still observed in shake flasks. In 7 L bioreactor, dissolved oxygen concentration controlled at more than 30% was helpful for improving the cell growth and the production of L-cysteine synthetase through regulating agitation rate and air flow rate during the middle and late stage.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ohmachi, Tetsuo; Nishino, Mizuka; Kawata, Maki; Edo, Namiko; Funaki, Hiroko; Narita, Megumi; Mori, Kazuyuki; Tamura, Yoshiharu; Asada, Yoshihiro published an article about the compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2,SMILESS:O=C(C1N=C(N)SC1)O ).Product Details of 2150-55-2. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:2150-55-2) through the article.

The newly isolated strain Pseudomonas sp. ON-4a converts D,L-2-amino-Δ2-thiazoline-4-carboxylic acid (D,L-ATC) to L-cysteine via N-carbamoyl-L-cysteine. A genomic DNA fragment from this strain containing the gene(s) encoding enzymes that convert D,L-ATC into L-cysteine was cloned in Escherichia coli. Transformants expressing cysteine-forming activity were selected by growth of an E. coli mutant defective in the cysB gene. A pos. clone, denoted CM1, carrying the plasmid pCM1 with an insert DNA of approx. 3.4 kb was obtained, and the nucleotide sequence of a complementing region was analyzed. Anal. of the sequence found two open reading frames, ORF1 and ORF2, which encoded proteins of 183 and 435 amino acid residues, resp. E. coli DH5α harboring pTrCM1, which was constructed by inserting the subcloned sequence into an expression vector, expressed two proteins of 25 kDa and 45 kDa. From the analyses of crude extracts of E. coli DH5α carrying deletion derivatives of pTrCM1 by sodium dodecyl sulfatepolyacrylamide gel electrophoresis and by enzymic activity, it was found that the 25-kDa protein encoded by ORF1 was the enzyme L-2-amino-Δ2-thiazoline-4-carboxylic acid hydrolase, which catalyzes the conversion of D,L-ATC to N-carbamoyl-L-cysteine, and that the 45-kDa protein encoded by ORF2 was the enzyme N-carbamoyl-L-cysteine amidohydrolase, which catalyzes the conversion of N-carbamoyl-L-cysteine to L-cysteine.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Computed Properties of C4H6N2O2S. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Microbial enzyme conversion of L-cysteine and L-cystine. Author is Liu, Zhong; Yang, Wenbo; Bai, Gang; Tian, Wang; Jin, Yongjie.

Pseudomonas sp. TS1138 isolated from soil samples was able to form L-cysteine from DL-2-Amiuo-δ2-Thiazoline-4-Carboxylic Acid (DL-ATC) after cultured 16 h. The optimum carbon and nitrogen sources of strain growth and enzyme formation are glucose and urea. This enzyme was induced by DL-ATC. The product was identified to be L-Cysteine based on thin layer chromatog., optical rotation and HPLC studies.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Amino-2-fluoropyridine( cas:1827-27-6 ) is researched.Recommanded Product: 1827-27-6.Wu, Jing-wei; Yin, Ling; Liu, Yu-qiang; Zhang, Huan; Xie, Ya-fei; Wang, Run-ling; Zhao, Gui-long published the article 《Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout》 about this compound( cas:1827-27-6 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: bromonaphthylmethyltriazolyl thioether preparation URAT1 inhibitor; structure bromonaphthylmethyltriazolyl thioether inhibition uric acid transporter; pharmacophore determination bromonaphthylmethyltriazolyl thioether URAT1 inhibition QSAR; 3D-QSAR; Bioisosteres; Biological evaluation; Gout; Synthesis. Let’s learn more about this compound (cas:1827-27-6).

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC50 value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-Acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-Methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789), published in 2012-05-24, which mentions a compound: 91912-53-7, Name is 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, Molecular C8H8N4, Application In Synthesis of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine.

Alpha-7 nicotinic acetylcholine receptors (α7 nAChR) are implicated in the modulation of many cognitive functions such as attention, working memory, and episodic memory. For this reason, α7 nAChR agonists represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer’s disease (AD) and schizophrenia. A medicinal chem. effort, around our previously reported chem. series, permitted the discovery of a novel class of α7 nAChR agonists with improved selectivity, in particular against the α3 receptor subtype and better ADME profile. The exploration of this series led to the identification of 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide [(I), SEN15924, WAY-361789], a novel, full agonist of the α7 nAChR that was evaluated in vitro and in vivo. Compound I proved to be potent and selective, and it demonstrated a fair pharmacokinetic profile accompanied by efficacy in rodent behavioral cognition models (novel object recognition and auditory sensory gating).

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem