Interesting scientific research on Pyrazine-2-carboxylic acid

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An article The crystal structures of the ligand N-(quinolin-8-yl) pyrazine-2-carboxamide and of a tetranuclear copper(II) complex WOS:000477632400011 published article about CU-II COMPLEX; MOLECULAR-STRUCTURE; MAGNETIC-PROPERTIES in [Cati, Dilovan S.] Debiopharm Int SA, Chemin Messidor 5-7,CP 5911, CH-1002 Lausanne, Switzerland; [Stoeckli-Evans, Helen] Univ Neuchatel, Inst Phys, Rue Emile Argand 11, CH-2000 Neuchatel, Switzerland in 2019, Cited 31. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: 98-97-5

The title tridentate ligand, C14H10N4O, N-(quinolin-8-yl) pyrazine-2-carboxamide (HL1), crystallizes with three independent molecules (A, B and C) in the asymmetric unit. All three molecules are relatively planar (r.m.s. deviations are 0.068, 0.055 and 0.06 angstrom, respectively), with the NH H atom forming three-centered (bifurcated) intramolecular N-H center dot center dot center dot N hydrogen bonds in each molecule. There is also an intramolecular C-H center dot center dot center dot O contact present in each molecule, involving the benzene ring of the quinoline unit and the amide carboxamide O atom. In the crystal, the three molecules stack in columns with the various molecules being linked by offset pi-pi interactions [intercentroid distances vary from 3.367 (5) to 3.589 (5) angstrom], forming layers parallel to the ab plane. The title complex, [Cu-4(C42H44N8O16)]center dot 2CH(3)OH, {hexa-mu-acetato-1: 2 kappa O-2:O’;2:3 kappa O-8:O’;3:4 kappa O-2:O’-dimethanol-1 kappa O, 2 kappa O-bis[N-(quinolin-8-yl) pyrazine-2-carboxamide]-1 kappa N-3, N’, N ”; 4 kappa(3) N, N’, N ”-tetracopper(II) methanol disolvate} (I), was obtained by the reaction of HL1 with Cu(CH3CO2)(2). It consists of a tetranuclear complex with a central tetrakis(mu-acetato) dicopper paddle-wheel moiety linked on either side via bridging acetato ions to a mononuclear copper(II)-(L1) complex; it crystallizes as a methanol disolvate. The complex possesses inversion symmetry, being located about a center of symmetry situated at the mid-point of the Cu center dot center dot center dot Cu bond of the paddle-wheel moiety. In the crystal, the complex molecules are linked by O-H center dot center dot center dot O hydrogen bonds, forming chains along the [01 (1) over bar] direction, which are linked by offset pi-pi interactions [intercentroid distance = 3.7367 (11) angstrom] and C-H center dot center dot center dot O hydrogen bonds, leading to the formation of a supramolecular framework.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

A new application aboutPyrazine-2-carboxylic acid

Welcome to talk about 98-97-5, If you have any questions, you can contact Singh, P; Babu, SA; Aggarwal, Y; Patel, P or send Email.. SDS of cas: 98-97-5

I found the field of Chemistry very interesting. Saw the article Pd(II)-catalyzed, Picolinamide-aided sp(2) gamma-C-H Functionalization of Phenylglycinol: Access to gamma-C-H Arylated, Alkylated and Halogenated Phenylglycinol Scaffolds published in 2021. SDS of cas: 98-97-5, Reprint Addresses Babu, SA (corresponding author), Indian Inst Sci Educ & Res IISER Mohali, Dept Chem Sci, Sect 81, Manauli Po 140306, Punjab, India.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

We report the Pd(II)-catalyzed picolinamide-aided ortho-C-H arylation-, alkylation-, and halogenation (sp(2) gamma-C-H functionalization) of phenylglycinol substrates. Phenylglycinols are remarkable building blocks and have found different applications in synthetic organic and medicinal chemistry. This work is a contribution towards the expansion of the library of phenylglycinol scaffolds and also substrate scope development by using the Pd(II)-catalyzed bidentate directing group picolinamide-aided C-H activation tactic.

Welcome to talk about 98-97-5, If you have any questions, you can contact Singh, P; Babu, SA; Aggarwal, Y; Patel, P or send Email.. SDS of cas: 98-97-5

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An overview of features, applications of compound:Pyrazine-2-carboxylic acid

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In 2020 J THERM ANAL CALORIM published article about PHARMACEUTICAL COCRYSTALS; SALTS; DESIGN; POLYMORPHISM; INVESTIGATE; SOLUBILITY; STABILITY; BEHAVIOR; COFORMER; LIQUID in [de Almeida, Amanda Cosmo; Ferreira, Patricia Osorio; Ekawa, Bruno; Sobral Carvalho, Ana Carina; Caires, Flavio Junior] Sao Paulo State Univ, Inst Chem, UNESP, Araraquara, Brazil; [Torquetti, Carolina; dos Santos, Everton Carvalho; Caires, Flavio Junior] Sao Paulo State Univ, Sch Sci, UNESP, Bauru, Brazil in 2020, Cited 52. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Quality Control of Pyrazine-2-carboxylic acid

Novel cocrystals of ciprofloxacin with pyrazinoic acid and p-aminobenzoic acid in the 1:1 stoichiometric ratio were obtained by the mechanochemical method, under conditions of liquid-assisted grinding (LAG/ethanol) and neat grinding. They were characterized by powder X-ray diffractometry, infrared spectroscopy, simultaneous thermogravimetry, differential thermal analysis, differential scanning calorimetry (DSC) and DSC-Microscopy system. The results confirmed the successful synthesis of the cocrystals and indicated the functional groups responsible for the formation of the new supramolecular synthons. In addition, from the thermal analysis, it was possible to evaluate the thermal stability, composition, crystallization processes during heating, polymorphic transitions and construct the binary phase diagrams.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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An article Novel coumarin-isatin hybrids as potent antileishmanial agents: Synthesis, in silico and in vitro evaluations WOS:000647574400008 published article about LEISHMANIA; INFECTION; DOCKING in [Khatoon, Saira; Hameed, Shahid; Naseer, Muhammad Moazzam] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan; [Aroosh, Aiman; Islam, Arshad; Kalsoom, Saima; Yasinzai, Masoom] Int Islamic Univ, Fac Basic & Appl Sci, Suleiman Bin Abdullah Aba Akhail Ctr Interdiscipl, Islamabad 44000, Pakistan; [Islam, Arshad] Govt Lady Reading Hosp Med Teaching Inst, Dept Pathol, Peshawar, KPK, Pakistan; [Ahmad, Faisal] Quaid I Azam Univ, Natl Ctr Bioinformat, Islamabad 45320, Pakistan; [Abbasi, Sumra Wajid] Natl Univ Med Sci, Dept Biol Sci, Rawalpindi, Pakistan in 2021, Cited 48. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

Leishmaniasis being one of the six major tropical diseases that affects nearly 0.7-1.3 million people annually, has so far limited and high toxic therapeutic options. Herein, we report the synthesis, in silico, and in vitro evaluations of novel coumarin-incorporated isatin hydrazones (Spf-1 – Spf-10) as highly potent and safe antileishmanial agents. Molecular docking was initially carried out to decipher the binding confirmation of lead molecules towards the active cavity of the target protein (Leishmanolysin gp63) of Leishmania tropica. Among all the docked compounds, only Spf-6, Spf-8, and Spf-10 showed high binding affinities due to a pattern of strong conventional hydrogen bonds and hydrophobic pi-interactions. The molecular dynamics simulations showed the stable pattern of such bonding and structure-based confirmation with a time scale of 50 ns towards the top compound (Spf-10) and protein. These analyses affirmed the high stability of the system. Three out of ten compounds evaluated for their antileishmanial activity against Leishmania tropica promastigotes and amastigotes were found to be active at micromolar concentrations (IC50 range 0.1-4.13 mu mol/L), and most importantly, they were also found to be highly biocompatible when screened for their toxicity in human erythrocytes.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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Kashid, BB; Ghanwat, AA; Khedkar, VM; Dongare, BB; Shaikh, MH; Deshpande, PP; Wakchaure, YB in [Kashid, Bharat B.; Ghanwat, Anil A.; Dongare, Balasaheb B.] Solapur Univ, Sch Chem Sci, Chem Res Lab, Solapur 413255, MS, India; [Khedkar, Vijay M.] Shri Vile Parle Kelavani Mandals Inst Pharm, Dept Pharmaceut Chem, Dhule 424001, MS, India; [Shaikh, Mubarak H.; Deshpande, Prathmesh P.; Wakchaure, Yogesh B.] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, MS, India published Design, Synthesis, In Vitro Antimicrobial, Antioxidant Evaluation, and Molecular Docking Study of Novel Benzimidazole and Benzoxazole Derivatives in 2019, Cited 52. Computed Properties of C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A series of novel 2-substituted benzimidazole and benzoxazole derivatives as a potential antimicrobial and antioxidant agent were synthesized via coupling of N-methyl-o-phenylenediamine or 2-amino-phenol with aromatic aldehyde and acid in the presence of polyphosphoric acid as an efficient catalyst as well as solvent by conventional method in short reaction times with excellent yield. The newly synthesized benzimidazole and benzoxazole derivatives were evaluated for antimicrobial and antioxidant activity and exhibited excellent to good activities compared to the standard drugs. Furthermore, the theoretical predictions based on molecular docking against microbial DNA gyrase could provide an insight into the plausible mechanism of action and establish a link between the observed antimicrobial activity and the binding affinity shedding light on specific thermodynamic (bonded and nonbonded) interactions governing the activity. Furthermore, the synthesized compounds were analyzed for absorption, distribution, metabolism, and excretion properties and exhibited potential properties to build up as good oral drug candidates.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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Welcome to talk about 98-97-5, If you have any questions, you can contact Etaiw, SEH; Marie, H; Shalaby, EM; Farag, RS; Elsharqawy, FA or send Email.. Safety of Pyrazine-2-carboxylic acid

An article Sensing and photocatalytic properties of nanosized Cu(I)CN organotin supramolecular coordination polymer based on pyrazine WOS:000478695400001 published article about METAL-ORGANIC FRAMEWORKS; X-RAY-STRUCTURE; CRYSTAL-STRUCTURES; COPPER(I) CYANIDE; ETHYL ISONICOTINATE; SELECTIVE DETECTION; LUMINESCENT SENSOR; ANTITUMOR-ACTIVITY; BUILDING-BLOCKS; SINGLE-CRYSTAL in [Etaiw, Safaa El-din H.; Marie, Hassan; Elsharqawy, Fatma A.] Tanta Univ, Fac Sci, Chem Dept, Tanta, Egypt; [Shalaby, Elsayed M.] Natl Res Ctr, Phys Div, Xray Crystallog Lab, Cairo, Egypt; [Farag, Rabie S.] Al Azhar Univ, Fac Sci, Chem Dept, Cairo, Egypt in 2019, Cited 76. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Safety of Pyrazine-2-carboxylic acid

Orange prismatic crystals of the supramolecular coordination polymer (SCP) (3)(infinity)[Cu(CN)(2)(Me3Sn)(Pyz)], SCP1, were synthesized using a self-assembly method under ambient conditions. Nanosized 1 was obtained using the same molar ratio in water by ultrasonic irradiation. SCP1 was characterized using single-crystal X-ray diffraction, elemental analysis, thermal analysis and Fourier transform infrared spectroscopy. SCP1 and its nanosized 1 particles were also examined using powder X-ay diffraction and scanning electron microscopy. The luminescence emission of SCP1 was studied as well as its use as a sensor for the detection of common organic solvents and metal ions. Also, the catalytic activities of nanosized 1 towards various organic dyes were investigated under ambient conditions, UV irradiation and ultrasonic irradiation. Nanosized 1 as a heterogeneous nanoparticle catalyst exhibits high catalytic activity for the degradation of eosin-Y and acid blue dyes. The mechanism of degradation investigated using various scavenger techniques is proposed and discussed. The catalytic oxidation process is mainly caused by center dot OH radicals.

Welcome to talk about 98-97-5, If you have any questions, you can contact Etaiw, SEH; Marie, H; Shalaby, EM; Farag, RS; Elsharqawy, FA or send Email.. Safety of Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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An article SAR Studies Leading to the Identification of a Novel Series of Metallo-beta-lactamase Inhibitors for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections That Display Efficacy in an Animal Infection Model WOS:000456349300014 published article about PSEUDOMONAS-AERUGINOSA; ACID in [Leiris, Simon; Coelho, Alicia; Castandet, Jerome; Bayet, Maelle; Lozano, Clarisse; Bougnon, Juliette; Bousquet, Justine; Everett, Martin; Lemonnier, Marc; Sprynski, Nicolas; Zalacain, Magdalena; Davies, David T.] Antabio SAS, 436 Rue Pierre & Marie Curie, F-31670 Labege, France; [Zalacain, Magdalena] Zala Drug Discovery Consulting LLC, W Chester, PA 19380 USA; [Pallin, Thomas David; Cramp, Michael C.; Jennings, Neil; Raphy, Gilles; Jones, Mark W.] 8 9 Spire Green Ctr, Charles River Labs, Harlow CM19 5TR, Essex, England; [Pattipati, Ramesh; Shankar, Battu; Sivasubrahmanyam, Relangi; Soodhagani, Ashok K.; Juventhala, Ramakrishna R.; Pottabathini, Narender; Pothukanuri, Srinivasu] GVK Biosci Private Ltd, Plot 28 A,IDA Nacharam, Hyderabad 500076, India; [Benvenuti, Manuela; Pozzi, Cecilia; Mangani, Stefano] Univ Siena, Dept Biotechnol Chem & Pharm, 2 Via Aldo Moro, I-53100 Siena, Italy; [De Luca, Filomena; Cerboni, Giulia; Docquier, Jean-Denis] Univ Siena, Dept Med Biotechnol, 16 Viale Bracci, I-53100 Siena, Italy; [Pottabathini, Narender] Laurus Labs Ltd, Plot DS1,IKP Knowledge Pk, Hyderabad 500078, Telangana, India in 2019, Cited 24. Recommanded Product: Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-beta-lactamase (MBL) and serine-beta-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new beta-lactamase inhibitors to be used in conjunction with carbapenems and other beta-lactam antibiotics. Herein, we describe our initial exploration of a novel chemical series of metallo-beta-lactamase inhibitors, from concept to efficacy, in a survival model using an advanced tool compound (ANT431) in conjunction with meropenem.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Awesome Chemistry Experiments For 98-97-5

Welcome to talk about 98-97-5, If you have any questions, you can contact Korff, M; Imberg, L; Will, JM; Buckreiss, N; Kalinina, SA; Wenzel, BM; Kastner, GA; Daniliuc, CG; Barth, M; Ovsepyan, RA; Butov, KR; Humpf, HU; Lehr, M; Panteleev, MA; Poso, A; Karst, U; Steinmetzer, T; Bendas, G; Kalinin, DV or send Email.. Application In Synthesis of Pyrazine-2-carboxylic acid

Authors Korff, M; Imberg, L; Will, JM; Buckreiss, N; Kalinina, SA; Wenzel, BM; Kastner, GA; Daniliuc, CG; Barth, M; Ovsepyan, RA; Butov, KR; Humpf, HU; Lehr, M; Panteleev, MA; Poso, A; Karst, U; Steinmetzer, T; Bendas, G; Kalinin, DV in AMER CHEMICAL SOC published article about in [Korff, Marvin; Imberg, Lukas; Kastner, Gregor A.; Barth, Maximilian; Lehr, Matthias; Kalinin, Dmitrii, V] Univ Munster, Inst Pharmaceut & Med Chem, D-48149 Munster, Germany; [Will, Jonas M.; Karst, Uwe] Univ Munster, Inst Inorgan & Analyt Chem, D-48149 Munster, Germany; [Bueckreiss, Nico; Bendas, Gerd] Univ Bonn, Pharmaceut Inst, D-53121 Bonn, Germany; [Kalinina, Svetlana A.; Humpf, Hans-Ulrich] Univ Munster, Inst Food Chem, D-48149 Munster, Germany; [Wenzel, Benjamin M.; Steinmetzer, Torsten] Philipps Univ Marburg, Inst Pharmaceut Chem, Dept Pharm, D-35032 Marburg, Germany; [Daniliuc, Constantin G.] Univ Munster, Inst Organ Chem, D-48149 Munster, Germany; [Ovsepyan, Ruzanna A.; Butov, Kirill R.; Panteleev, Mikhail A.] Dmitriy Rogachev Natl Med Res Ctr Pediat Hematol, Lab Translat Med, Moscow 117997, Russia; [Ovsepyan, Ruzanna A.; Butov, Kirill R.; Panteleev, Mikhail A.] Russian Acad Sci, Ctr Theoret Problems Physicochem Pharmacol, Moscow 119991, Russia; [Panteleev, Mikhail A.] Lomonosov Moscow State Univ, Fac Phys, Moscow 119991, Russia; [Panteleev, Mikhail A.] Moscow Inst Phys & Technol, Fac Biol & Med Phys, Dolgoprudnyi 141700, Russia; [Poso, Antti] Univ Eastern Finland, Fac Hlth Sci, Sch Pharm, Kuopio 70211, Finland; [Poso, Antti] Univ Hosp Tubingen, Dept Internal Med 8, D-72076 Tubingen, Germany in 2020, Cited 75. Application In Synthesis of Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

We herein report the conventional and microscale parallel synthesis of selective inhibitors of human blood coagulation factor XIIa and thrombin exhibiting a 1,2,4-triazol-5-amine scaffold. Structural variations of this scaffold allowed identifying derivative 21i, a potent 29 nM inhibitor of FXIIa, with improved selectivity over other tested serine proteases and also finding compound 21m with 27 nM inhibitory activity toward thrombin. For the first time, acylated 1,2,4-triazol-5-amines were proved to have anticoagulant properties and the ability to affect thrombin- and cancer-cell-induced platelet aggregation. Performed mass spectrometric analysis and molecular modeling allowed us to discover previously unknown interactions between the synthesized inhibitors and the active site of FXIIa, which uncovered the mechanistic details of FXIIa inhibition. Synthesized compounds represent a promising starting point for the development of novel antithrombotic drugs or chemical tools for studying the role of FXIIa and thrombin in physiological and pathological processes.

Welcome to talk about 98-97-5, If you have any questions, you can contact Korff, M; Imberg, L; Will, JM; Buckreiss, N; Kalinina, SA; Wenzel, BM; Kastner, GA; Daniliuc, CG; Barth, M; Ovsepyan, RA; Butov, KR; Humpf, HU; Lehr, M; Panteleev, MA; Poso, A; Karst, U; Steinmetzer, T; Bendas, G; Kalinin, DV or send Email.. Application In Synthesis of Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

A new application aboutPyrazine-2-carboxylic acid

Quality Control of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Samie, A; Salimi, A or send Email.

Quality Control of Pyrazine-2-carboxylic acid. In 2019 CRYSTENGCOMM published article about HYDROGEN-BOND; CRYSTAL-STRUCTURES; MODEL ENERGIES; SOLID FORMS; PHASE; SALTS; COCRYSTALS; DRUG; ACCURATE; ACID in [Samie, Ali; Salimi, Alireza] Ferdowsi Univ Mashhad, Fac Sci, Dept Chem, Mashhad, Razavi Khorasan, Iran in 2019, Cited 67. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

On the basis of crystal engineering, two similar esters of phenyl pyridine-2-carboxylate (I) and phenyl pyrazine-2-carboxylate (II) were designed and synthesized. The compounds were characterized using FT-IR, mass spectrometry, CHN-elemental analyses, NMR and PXRD. For each compound, two polymorphs were obtained (Ia, Ib and IIa, IIb) and identified by TGA, DSC and SCXRD. A comparison of the crystal structures of the polymorphs revealed that the different torsion angles of the pyrazine (tau(1)) and phenyl (tau(2)) rings to the ester backbone resulted in the conformers I and II, respectively. Theoretical criteria (max(Delta theta), rmsd[r]-crystal, energy profile) confirmed that the structural differences in the conformers are in the range of acceptable values for the detection of conformational changes. The phase stability of the polymorphs was investigated by slurry and grinding methods as well as by the HSM technique. Since the orientations of pyrazine and phenyl moieties were altered in the polymorphs, the hydrogen bond donor and acceptors exhibited meaningful supramolecular architectures in the crystal packing as well as C-HMIDLINE HORIZONTAL ELLIPSISN, C-HMIDLINE HORIZONTAL ELLIPSISO and C-HMIDLINE HORIZONTAL ELLIPSIS pi interactions. The energetic study of the noncovalent interactions in the molecular pairs (dimers) of the polymorph crystal structures was performed by DFT-D calculations.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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Safety of Pyrazine-2-carboxylic acid. Recently I am researching about ACTIVATION, Saw an article supported by the NIA of the NIH [R01AG058673]; Alzheimer’s Drug Discovery Foundation [20150601]; Commonwealth of Virginia’s Alzheimer’s and Related Disease Research Award Fund [18-2]; NATIONAL INSTITUTE ON AGINGUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute on Aging (NIA) [R01AG058673] Funding Source: NIH RePORTER. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Jiang, YQ; He, L; Green, J; Blevins, H; Guo, CQ; Patel, SH; Halquist, MS; Mcrae, M; Venitz, J; Wang, XY; Zhang, SJ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

NLRP3 inflammasomes have recently emerged as an attractive drug target for neurodegenerative disorders. In our continuing studies, a new chemical scaffold was designed as selective inhibitors of NLRP3 inflammasomes. Initial characterization of the lead HL16 demonstrated improved, however, nonselective inhibition on the NLRP3 inflammasome. Structure-activity relationship studies of HL16 identified a new lead, 17 (YQ128), with an IC50 of 0.30 +/- 0.01 mu M. Further studies from in vitro and in vivo models confirmed its selective inhibition on the NLRP3 inflammasome and its brain penetration. Furthermore, pharmacokinetic studies in rats at 20 mg/kg indicated extensive systemic clearance and tissue distribution, leading to a half-life of 6.6 h. However, the oral bioavailability is estimated to be only 10%, which may reflect limited GI permeability and possibly high first-pass effects. Collectively, these findings strongly encourage development of more potent analogues with improved pharmacokinetic properties from this new chemical scaffold.

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Jiang, YQ; He, L; Green, J; Blevins, H; Guo, CQ; Patel, SH; Halquist, MS; Mcrae, M; Venitz, J; Wang, XY; Zhang, SJ or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem