Category: Pyrazines

Formula: C5H4N2O2. In 2020 J MATER CHEM B published article about SENSITIVE FLUORESCENT-PROBE; HSA; SENSOR; RECOGNITION; SITE; QUANTIFICATION; FLUOROPHORES; DIAGNOSIS; INSIGHTS; BINDING in [Wang, Zhi-Gang; Yan, Xiao-Jing; Xie, Cheng-Zhi; Xu, Jing-Yuan] Tianjin Med Univ, Sch Pharm, Dept Chem Biol, Tianjin 300070, Peoples R China; [Wang, Zhi-Gang; Yan, Xiao-Jing; Xie, Cheng-Zhi; Xu, Jing-Yuan] Tianjin Med Univ, Sch Pharm, Tianjin Key Lab Technol Enabling Dev Clin Therape, Tianjin 300070, Peoples R China; [Liu, Hai-Bo] Chinese Acad Med Sci, Peking Union Med Coll, Inst Med Plant Dev, Beijing 100193, Peoples R China; [Zhang, De-Long] Tianjin Santan Hosp, Dept Pharm, Tianjin 300193, Peoples R China; [Liu, Wei] Tianjin Med Univ, Hosp 2, Tianjin 300211, Peoples R China; [Li, Qing-Zhong] Yantai Univ, Sch Chem & Chem Engn, Lab Theoret & Computat Chem, Yantai 264005, Peoples R China in 2020, Cited 53. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Human serum albumin (HSA) is considered as a biomarker for the early diagnosis of renal disease, therefore identifying and detecting HSA in biological fluids (especially urine) with an easy method is of great importance. Herein, we report a novel hydrazide Schiff base fluorescent probeN ‘-((7-(diethylamino)-2-oxo-2H-chromen-3-yl)methylene)pyrazine-2-carbohydrazide (NPC), which self-assembled into nanoparticles in aqueous solution. Based on disassembly-induced emission and the site-specific recognition mechanism, the binding ofNPCwith HSA resulted in a fluorescence turn-on response. ProbeNPCexhibited superior selectivity and sensitivity toward HSA with a detection limit of 0.59 mg L(-1)in PBS and 0.56 mg L(-1)in the urine sample. The site-binding mechanism ofNPCwith HSA was explored by fluorescence quenching study, Job’s plot analysis, HSA destruction, site marker displacement and molecular docking. Fluorescence imaging of HSA in MCF-7 cells was achieved by using a non-toxicNPCprobe, suggesting thatNPCcould be applied to visualize the level of HSAin vivo. More importantly, further practical applications of probeNPCin human urine samples were achieved with satisfactory results by using a fluorometer or test paper, which could provide extensive application in clinical diagnosis.

Welcome to talk about 98-97-5, If you have any questions, you can contact Wang, ZG; Yan, XJ; Liu, HB; Zhang, DL; Liu, W; Xie, CZ; Li, QZ; Xu, JY or send Email.. Formula: C5H4N2O2

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

Application In Synthesis of Pyrazine-2-carboxylic acid. In 2020 EUR J MED CHEM published article about NONCOVALENT; APOPTOSIS; PATHWAY; POTENT in [Sun, Qi; Zhou, Tongliang; Xi, Dandan; Li, Xiaona; Lu, Zirui; Xu, Fengrong; Wang, Chao; Niu, Yan; Xu, Ping] Peking Univ, Sch Pharmaceut Sci, Dept Med Chem, Hlth Sci Ctr, Beijing 100191, Peoples R China; [Sun, Qi] Peking Univ, Coll Chem & Mol Engn, State Key Lab Struct Chem Unstable & Stable Speci, BNLMS, Beijing 100871, Peoples R China in 2020, Cited 31. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A series of tripeptidic proteasome inhibitors with furylketone as C-terminus were designed and synthesized. Biochemical evaluations against beta 1, beta 2 and beta 5 subunits revealed that they acted selectively on beta 5 subunit with IC(50)s against chymotrypsin-like (CT-L) activity in micromolar range. LC-MS/MS analysis of the ligand-20S proteasome mixture showed that the most potent compound 11m (IC50 = 0.18 mu M) made no covalent modification on 20S proteasome. However, it was identified acting in a slowly reversible manner in wash-out assay and the reversibility was much lower than that of MG132, suggesting the possibility of these tripeptidic furylketones forming reversible covalent bonds with 20S proteasome. Several compounds were selected for anti-proliferative assay towards multiple cancer cell lines, and compound 11m displayed comparable potency to positive control (MG132) in all cell lines tested. Furthermore, the pharmacokinetic (PK) data in rats indicated 11m behaved similarly (C-max, 2007 mu g/L; AUC(0-t), 680 mu g/L.h; V-ss, 0.66 L/kg) to the clinical used agent carfilzomib. All these data suggest 11m is a good lead compound to be developed to novel anti-tumor agent. (c) 2020 Elsevier Masson SAS. All rights reserved.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P or send Email.

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

Application In Synthesis of Pyrazine-2-carboxylic acid. Omondi, RO; Sibuyi, NRS; Fadaka, AO; Meyer, M; Jaganyi, D; Ojwach, SO in [Omondi, Reinner O.; Ojwach, Stephen O.] Univ KwaZulu Natal, Sch Chem & Phys, Private Bag X01, ZA-3209 Pietermaritzburg, South Africa; [Sibuyi, Nicole R. S.; Fadaka, Adewale O.; Meyer, Mervin] Univ Western Cape, Dept Biotechnol, Bag X17, ZA-7535 Cape Town, South Africa; [Jaganyi, Deogratius] Mt Kenya Univ, Sch Pure & Appl Sci, POB 342-01000, Thika, Kenya; [Jaganyi, Deogratius] Durban Univ Technol, Fac Sci Appl, Dept Chem, POB 1334, ZA-4000 Durban, South Africa published Role of pi-conjugation on the coordination behaviour, substitution kinetics, DNA/BSA interactions, and in vitro cytotoxicity of carboxamide palladium(II) complexes in 2021, Cited 70. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Treatments of N-(pyridin-2-ylmethyl)pyrazine-2-carboxamide (L-1), N-(quinolin-8-yl)pyrazine-2-carboxamide (L-2), N-(quinolin-8-yl)picolinamide (L-3) and N-(quinolin-8-yl)quinoline-2-carboxamide (L-4) with [PdCl2(NCMe)](2) afforded the corresponding Pd(ii) complexes, [Pd(L-1)Cl] (PdL1); [Pd(L-2)Cl] (PdL2); [Pd(L-3)Cl] (PdL3); and [Pd(L-4)Cl] (PdL4) in moderate yields. Structural characterisation of the compounds was achieved by NMR and FT-IR spectroscopies, elemental analyses and single crystal X-ray crystallography. The solid-state structures of complexes PdL2-PdL4 established the presence of one tridentate carboxamide and Cl ligands around the Pd(ii) coordination sphere, to give distorted square planar complexes. Electrochemical investigations of PdL1-PdL4 showed irreversible one-electron oxidation reactions. Kinetics reactivity of the complexes towards bio-molecules, thiourea (Tu), l-methionine (L-Met) and guanosine 5 ‘-diphosphate disodium salt (5 ‘-GMP) decreased in the order: PdL1 > PdL2 > PdL3 > PdL4, in tandem with the density functional theory (DFT) data. The complexes bind favourably to calf thymus (CT-DNA), and bovine serum albumin (BSA), and the order of their interactions agrees with the substitution kinetics trends. The in vitro cytotoxic activities of PdL1-PdL4 were examined in cancer cell lines A549, PC-3, HT-29, Caco-2, and HeLa, and a normal cell line, KMST-6. Overall, PdL1 and PdL3 displayed potent cytotoxic effects on A549, PC-3 HT-29 and Caco-2 comparable to cisplatin. All the investigated complexes exhibited lower toxicity on normal cells than cisplatin.

Application In Synthesis of Pyrazine-2-carboxylic acid. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.

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

Application In Synthesis of Pyrazine-2-carboxylic acid. In 2019 J MED CHEM published article about ACTIVATION in [Jiang, Yuqi; He, Liu; Green, Jakob; Blevins, Hallie; Zhang, Shijun] Virginia Commonwealth Univ, Dept Med Chem, Richmond, VA 23298 USA; [Guo, Chunqing; Wang, Xiang-Yang] Virginia Commonwealth Univ, Dept Human & Mol Genet, Richmond, VA 23298 USA; [Patel, Sulay Harsiddhbhai; McRae, MaryPeace] Virginia Commonwealth Univ, Dept Pharmacotherapy & Outcomes, Richmond, VA 23298 USA; [Halquist, Matthew S.; Venitz, Jurgen] Virginia Commonwealth Univ, Dept Pharmaceut, Richmond, VA 23298 USA; [Jiang, Yuqi] Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Shandong, Peoples R China in 2019, Cited 30. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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.

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

COA of Formula: C5H4N2O2. In 2020 BIOORG MED CHEM LETT published article about PHARMACOLOGICAL EVALUATION; ANTIBACTERIAL ACTIVITY; ANTIMICROBIAL ACTIVITY; ACCURATE DOCKING; OXAZOLIDINONE; OXADIAZOLES; DESIGN; GLIDE in [Kashid, Bharat B.; Salunkhe, Pravin H.; Dongare, Balasaheb B.; Ghanwat, Anil A.] Solapur Univ, Sch Chem Sci, Chem Res Lab, Solapur 413255, India; [Salunkhe, Pravin H.] CSIR Natl Chem Lab, Dr Homi Bhabha Rd, Pune 411008, Maharashtra, India; [More, Kishor R.] Shandong Keyuan Pharmaceut Co Ltd, Keyuan St, Jinan, Shandong, Peoples R China; [Khedkar, Vijay M.] Vishwakarma Univ, Sch Pharm, Survey 2,3,4 Laxminagar, Pune 411048, Maharashtra, India in 2020, Cited 43. 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, 5-disubstituted 1, 3, 4-Oxadiazole derivatives as a potential anti-inflammatory, and antioxidant agent were synthesized via cyclisation. Hydrazide molecule treated with substituted acids in the presence of phosphorus oxychloride (POCl3) as an efficient reagent as well as solvent by conventional method with shorter reaction time and excellent yield. The newly synthesized 1, 3, 4-oxadiazole derivatives exhibited excellent to good anti-inflammatory and anti-oxidant activities compaired to the standard drugs. Molecular docking study on the crucial anti-inflammatory target-cyclooxygenase-2 (COX-2) revealed the ability of the scaffold to correctly recognize the active site and achieve significant bonded and non-bonded interactions with key residues therein. This study could identify potential compounds which can be pertinent starting points for structure-based drug design to obtain newer anti-inflammatory agents.

Welcome to talk about 98-97-5, If you have any questions, you can contact Kashid, BB; Salunkhe, PH; Dongare, BB; More, KR; Khedkar, VM; Ghanwat, AA or send Email.. COA of Formula: C5H4N2O2

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

Li, DD; Xu, QF; Li, YG; Qiu, YT; Ma, PT; Niu, JY; Wang, JP in [Li, Dandan; Xu, Qiaofei; Li, Yingguang; Qiu, Yueting; Ma, Pengtao; Niu, Jingyang; Wang, Jingping] Henan Univ, Coll Chem & Chem Engn, Inst Mol & Crystal Engn, Henan Key Lab Polyoxometalate Chem, Kaifeng 475004, Henan, Peoples R China published A Stable Polyoxometalate-Based Metal-Organic Framework as Highly Efficient Heterogeneous Catalyst for Oxidation of Alcohols in 2019, Cited 54. 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.

A novel copper-containing 3D polyoxometalate-based metal-organic framework (POMOF), H[(Cu5CuII)-Cu-I(pzc)(2)(pz)(4.5){P2W18O62}]center dot 6H(2)O (HENU-1, HENU = Henan University; Hpzc = pyrazine-2-carboxylic acid, pz = pyrazine), was successfully isolated by a one-step hydrothermal method. In this compound, the {P2W18} polyanion acts as a seven-connected linker bridging adjacent 2D double-layer networks, as well as a template to induce the formation of the desired 3D framework. Particularly, the pz ligands are generated from pzc ligands in situ during the reaction process. HENU-1 exhibits not only good stability in air but also tolerance to acidic and basic media. It was first employed as a highly efficient heterogeneous catalyst for the oxidation of 1-phenylethanol into acetophenone, which shows 97% yield using tert-butyl hydroperoxide as oxidant with a turnover frequency of up to 9690.h(-1), and was reused for at least five cycles without significant catalytic activity loss. No POM leaching or framework decomposition was observed in our study.

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

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. Application In Synthesis of Pyrazine-2-carboxylic acid, 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.

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

COA of Formula: C5H4N2O2. Reddyrajula, R; Dalimba, U in [Reddyrajula, Rajkumar; Dalimba, Udayakumar] Natl Inst Technol Karnataka, Dept Chem, Organ Chem Lab, Mangalore 575025, India published The bioisosteric modification of pyrazinamide derivatives led to potent antitubercular agents: Synthesis via click approach and molecular docking of pyrazine-1,2,3-triazoles in 2020, Cited 38. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Tuberculosis remains as a major public health risk which causes the highest mortality rate globally and an improved regimen is required to treat the drug-resistant strains. Pyrazinamide is a first-line antitubercular drug used in combination therapy with other anti-TB drugs. Herein, we describe the modification of pyrazinamide structure using bioisosterism and rational approaches by incorporating the 1,2,3-triazole moiety. Three sets of pyrazine-1,2,3-triazoles (3a-o, 5a-o and 9a-l) are designed, synthesized and evaluated for their in vitro inhibitory potency against mycobacterium tuberculosis H(37)Rv. The pyrazine-1,2,3-triazoles synthesized through the bioisosteric modification displayed improved activity as compared to rationally modified pyrazine-1,2,3-triazoles. Among 42 title compounds, seven derivatives demonstrated significant anti-tubercular activity with the MIC of 1.56 mu g/mL, which are two-fold more potent than the parent compound pyrazinamide. Further, the synthesized pyrazinamide analogs demonstrated moderate inhibition activity against several bacterial strains and possessed an acceptable in vitro cytotoxicity profile as well. Additionally, the activity profile of pyrazine-1,2,3-triazoles was validated by performing the molecular docking studies against the Inh A enzyme. Furthermore, in silico ADME prediction revealed good oral bioavailability for the potent molecules.

COA of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Reddyrajula, R; Dalimba, U or send Email.

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

In 2020 MOLECULES published article about MYCOBACTERIUM; DRUG; RESISTANCE; DELAMANID; DISCOVERY; MECHANISMS; INHIBITORS; ASSAY; Q203; BCG in [Brown, Alistair K.; Aljohani, Ahmed K. B.; Alsalem, Fatimah M. A.; Lu, Yucheng; Sellars, Jonathan D.] Newcastle Univ, Biosci Inst, Fac Med Sci, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England; [Broadhead, Joseph L.] Arcinova, Taylor Dr, Alnwick NE66 2DH, England; [Gill, Jason H.] Newcastle Univ, Fac Med Sci, Translat & Clin Res Inst, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England; [Gill, Jason H.; Sellars, Jonathan D.] Fac Med Sci, Sch Pharm, King George VI Bldg, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England in 2020, Cited 34. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. SDS of cas: 98-97-5

Discovery and development of new therapeutic options for the treatment of Mycobacterium tuberculosis (Mtb) infection, particularly drug-resistant strains, are urgently required to tackle the global burden of this disease. Herein, we reported the synthesis of a novel series of N-substituted amino acid hydrazides, utilising a scaffold hopping approach within a library of anti-tubercular agents. Efficacy and selectivity were evaluated against three strains of Mtb (wild-type, isoniazid-resistant and rifampicin-resistant), and cytotoxicity against macrophages in vitro. The antibacterial activity and therapeutic index of these molecules were significantly affected by modifications with the N-substituents. Introduction of a 3,5-dinitroaryl moiety demonstrated enhanced antibacterial activity against all three strains of Mtb. In contrast, the inclusion of an imidazo [1,2-a]pyridine-3-carboxy moiety resulted in enhanced activity towards isoniazid mono-resistant Mtb relative to wild-type Mtb. Consequently, this scaffold hopping approach showed significant promise for exemplification of novel molecules with specific activity profiles against drug-resistant tuberculosis.

Welcome to talk about 98-97-5, If you have any questions, you can contact Brown, AK; Aljohani, AKB; Alsalem, FMA; Broadhead, JL; Gill, JH; Lu, YC; Sellars, JD or send Email.. SDS of cas: 98-97-5

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

COA of Formula: C5H4N2O2. In 2019 J HETEROCYCLIC CHEM published article about ONE-POT SYNTHESIS; 2-SUBSTITUTED BENZOTHIAZOLES; OXIDATIVE CYCLIZATION; CATALYST; EFFICIENT; 2-ARYLBENZOXAZOLES; BASES 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 in 2019, Cited 52. 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.

COA of Formula: C5H4N2O2. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.

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