Pyrazines

Name: 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. 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.

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

HPLC of Formula: C5H4N2O2. In 2019 MOLECULES published article about SIGNALING PATHWAY; NATURAL-PRODUCTS; DERIVATIVES; APOPTOSIS; DESIGN; DISCOVERY; PREDICTION; CURCUMIN; ACID in [Wang, Jiawen; Liu, Tianjun] Tianjin Univ Tradit Chinese Med, Grad Inst, Tianjin 301617, Peoples R China; [Hong, Ge; Li, Guoliang; Wang, Wenzhi; Liu, Tianjun] Chinese Acad Med Sci & Peking Union Med Coll, Inst Biomed Engn, Tianjin Key Lab Biomed Mat, Tianjin 300192, Peoples R China; [Hong, Ge; Liu, Tianjun] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, 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.

Bivalent and polyvalent inhibitors can be used as antitumor agents. In this experiment, eight ligustrazine dimers and seven ligustrazine tetramers linked by alkane diamine with different lengths of carbon chain lengths were synthesized. After screening their antiproliferation activities against five cancer cell lines, most ligustrazine derivatives showed better cytotoxicity than the ligustrazine monomer. In particular, ligustrazine dimer 8e linked with decane-1,10-diamine exhibited the highest cytotoxicity in FaDu cells with an IC50 (50% inhibiting concentration) value of 1.36 nM. Further mechanism studies suggested that 8e could induce apoptosis of FaDu cells through the depolarization of mitochondrial membrane potential and S-phase cell cycle arrest. Inspired by these results, twenty-seven additional small molecule heterocyclic dimers linked with decane-1,10-diamine and nine cinnamic acid dimers bearing ether chain were synthesized and screened. Most monocyclic and bicyclic aromatic systems showed highly selective anti-proliferation activity to FaDu cells and low toxicity to normal MCF 10A cells. The structure-activity relationship revealed that the two terminal amide bonds and the alkyl linker with a chain length of 8-12 carbon were two important factors to maintain its antitumor activity. In addition, the ADMET calculation predicted that most of the potent compounds had good oral bioavailability.

HPLC 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

In 2021 DALTON T published article about COLON-CANCER CELLS; PLATINUM(II) COMPLEXES; MOLECULAR DOCKING; PT(II) COMPLEXES; BENIGN SYNTHESIS; DNA CLEAVAGE; CT-DNA; LIGANDS; BINDING; ANTICANCER 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 in 2021, Cited 70. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Product Details 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.

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

Category: Pyrazines. Authors Ma, JJ; Chen, SM; Bellotti, P; Guo, RY; Schafer, F; Heusler, A; Zhang, XL; Daniliuc, C; Brown, MK; Houk, KN; Glorius, F in AMER ASSOC ADVANCEMENT SCIENCE published article about in [Ma, Jiajia; Bellotti, Peter; Schafer, Felix; Heusler, Arne; Zhang, Xiaolong; Daniliuc, Constantin; Glorius, Frank] Westfalische Wilhelms Univ Munster, Organ Chem Inst, Corrensstr 40, D-48149 Munster, Germany; [Chen, Shuming; Houk, Kendall N.] Univ Calif Los Angeles, Dept Chem & Biochem, Los Angeles, CA 90095 USA; [Guo, Renyu; Brown, M. Kevin] Indiana Univ, Dept Chem, Bloomington, IN 47405 USA in 2021, Cited 74. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Dearomative cycloaddition reactions represent an ideal means of converting flat arenes into three-dimensional architectures of increasing interest in medicinal chemistry. Quinolines, isoquinolines, and quinazolines, despite containing latent diene and alkene subunits, are scarcely applied in cycloaddition reactions because of the inherent low reactivity of aromatic systems and selectivity challenges. Here, we disclose an energy transfer-mediated, highly regio- and diastereoselective intermolecular [4 + 2] dearomative cycloaddition reaction of these bicyclic azaarenes with a plethora of electronically diverse alkenes. This approach bypasses the general reactivity and selectivity issues, thereby providing various bridged polycycles that previously have been inaccessible or required elaborate synthetic efforts. Computational studies with density functional theory elucidate the mechanism and origins of the observed regio- and diastereoselectivities.

Welcome to talk about 98-97-5, If you have any questions, you can contact Ma, JJ; Chen, SM; Bellotti, P; Guo, RY; Schafer, F; Heusler, A; Zhang, XL; Daniliuc, C; Brown, MK; Houk, KN; Glorius, F or send Email.. Category: Pyrazines

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

Application In Synthesis of Pyrazine-2-carboxylic acid. In 2019 CHINESE J INORG CHEM published article about PHOTOLUMINESCENCE ENHANCEMENT; LIGANDS SYNTHESES; COMPLEXES; ACID; SERIES; TB; CONSTRUCTION; DESIGN; 3D-4F; GD in [Wang Yan; Chen Fei-Fei; Hu Xiao-Shuang; Zhao Ran; Chi Yu-Xian; Jin Jing] Liaoning Normal Univ, Sch Chem & Chem Engn, Dalian 116029, Liaoning, Peoples R China in 2019, Cited 42. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Using pyrazine-2-carboxylic acid (2-Hpzc), 3,5-pyridinedicarboxylic acid (3,5-H(2)PDA) and oxalic acid (H(2)ox) as ligands, nine Ag-Ln coordination polymers are synthesized by hydrothermal methods: {[LnAg(2-pzc)(2)(ox)]center dot H(2)ox} (Ln=Pr (1), Nd (2), Sm (3), Eu (4)), [LnAg(3,5-PDA)(ox)(H2O)](n), (Ln=Pr (5), Nd (6)), [LnAg(3,5-PDA)(3,5-HPDA)(ox)(0.5)(H2O)(2)](n) (Ln=Sm (7), Dy (8), Ho (9)). All of them possess the 3D network structure, i.e., coordination polymers 1 similar to 4 are isomorphic and connected by 2-pzc(-) and ox(2-), while coordination polymers 5 similar to 9 use 3,5-PDA(2-) and ox(2-) as bridging ligands. Photophysical properties of these coordination polymers are studied, and they show characteristic emissions of corresponding Ln(III) ions which should be attributed to the sensitization of the Agligand section (d-block). In addition, under the co-action of crystal field and 4d orbits of Ag(I) ion, the 4f orbits of Ln(III) ions are tuned and cause obvious shift of partial energy levels, which present shifts of the corresponding NIR emission bands and can be corroborated in their UV-Vis-NIR absorption spectra. CCDC: 1817276, 1; 1817247, 2; 1817248, 3; 1817249, 4; 1817251, 5; 1817255, 6; 1817269, 7; 1817280, 8; 1817285, 9.

Welcome to talk about 98-97-5, If you have any questions, you can contact Wang, Y; Chen, FF; Hu, XS; Zhao, R; Chi, YX; Jin, J or send Email.. Application In Synthesis of Pyrazine-2-carboxylic acid

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

Safety of Pyrazine-2-carboxylic acid. I found the field of Biochemistry & Molecular Biology very interesting. Saw the article Mycobacterium tuberculosis PanD Structure-Function Analysis and Identification of a Potent Pyrazinoic Acid-Derived Enzyme Inhibitor published in 2021, Reprint Addresses Gruber, G (corresponding author), Nanyang Technol Univ, Sch Biol Sci, Singapore 637551, Singapore.; Aldrich, CC (corresponding author), Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA.; Dick, T (corresponding author), Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA.; Dick, T (corresponding author), Hackensack Meridian Sch Med, Dept Med Sci, Nutley, NJ 07110 USA.; Dick, T (corresponding author), Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20007 USA.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

A common strategy employed in antibacterial drug discovery is the targeting of biosynthetic processes that are essential and specific for the pathogen. Specificity in particular avoids undesirable interactions with potential enzymatic counterparts in the human host, and it ensures ontarget toxicity. Synthesis of pantothenate (Vitamine B5), which is a precursor of the acyl carrier coenzyme A, is an example of such a pathway. In Mycobacterium tuberculosis (Mtb), which is the causative agent of tuberculosis (TB), pantothenate is formed by pantothenate synthase, utilizing D-pantoate and beta-Ala as substrates. beta-Ala is mainly formed by the decarboxylation of L-aspartate, generated by the decarboxylase PanD, which is a homo-oliogomer in solution. Pyrazinoic acid (POA), which is the bioactive form of the TB prodrug pyrazinamide, binds and inhibits PanD activity weakly. Here, we generated a library of recombinant Mtb PanD mutants based on structural information and PZA/POA resistance mutants. Alterations in oligomer formation, enzyme activity, and/or POA binding were observed in respective mutants, providing insights into essential amino acids for Mtb PanD’s proper structural assembly, decarboxylation activity and drug interaction. This information provided the platform for the design of novel POA analogues with modifications at position 3 of the pyrazine ring. Analogue 2, which incorporates a bulky naphthamido group at this position, displayed a 1000-fold increase in enzyme inhibition, compared to POA, along with moderately improved antimycobacterial activity. The data demonstrate that an improved understanding of mechanistic and enzymatic features of key metabolic enzymes can stimulate design of more-potent PanD inhibitors.

Welcome to talk about 98-97-5, If you have any questions, you can contact Ragunathan, P; Cole, M; Latka, C; Aragaw, WW; Hegde, P; Shin, J; Manimekalai, MSS; Rishikesan, S; Aldrich, CC; Dick, T; Gruber, G or send Email.. Safety of Pyrazine-2-carboxylic acid

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

In 2020 J MED CHEM published article about AUREUS STRESS TOLERANCE; STAPHYLOCOCCUS-AUREUS; PROTEASE; INSIGHTS; CLEAVAGE; REVEAL; ROLES in [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Sang, Zitai] Luoyang Normal Univ, Inst Life Sci, Luoyang 471934, Henan, 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. Recommanded Product: Pyrazine-2-carboxylic acid

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

Recommanded Product: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or send Email.

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

An article Synthesis of pyripyropene derivatives and their pest-control efficacy WOS:000512216500017 published article about ACYL-COA; ASPERGILLUS-FUMIGATUS; CHEMICAL-MODIFICATION; STRUCTURE ELUCIDATION; INHIBITORS; POTENT; RESISTANCE; METABOLITE in [Guro, Kimihiko; Horikoshi, Ryo; Nakamura, Satoshi; Mitomi, Masaaki; Oyama, Kazuhiko] Meiji Seika Pharma Co Ltd, Agr & Vet Div, Agr & Vet Res Labs, Kohoku Ku, 760 Morooka Cho, Yokohama, Kanagawa, Japan; [Hirose, Tomoyasu; Sunazuka, Toshiaki; Omura, Satoshi] Kitasato Univ, Kitasato Inst Life Sci, Grad Sch Infect Control Sci, Tokyo, Japan in 2019, Cited 22. 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

Pyripyropene A (PP-A), a secondary metabolite produced by filamentous fungi, shows insecticidal activity against agricultural insect pests. Synthesized PP derivatives also show a narrow insecticidal spectrum but high insecticidal activities against such sucking pests. PP-A has a low eco-toxicological impact and satisfies a prerequisite for next-generation insecticides. We investigated the effects of conversion of the 3-pyridyl and a-pyrone rings to other rings, as well as the effects of esterification, dehydration, and oxidization at the C-13 position in natural PP analogues, on the insecticidal activity and spectrum. The conversions of the 3-pyridyl and alpha-pyrone rings markedly reduced the insecticidal activity with a minimal impact on the spectrum, indicative of an important role for these rings in insecticidal activity. Some derivatives with modified structures at the C-13 position showed a higher inhibitory effect on the motility of canine heartworms and mosquito vectors than did PP-A, suggesting their utility as filaria control drugs.

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

Authors Zhao, YF; Wang, AL; Kang, J; Chu, HB; Zhang, HX; Zhao, YL in ELSEVIER SCIENCE SA published article about FLUORESCENCE; SILVER; SURFACE in [Zhao, Yanfang; Wang, Ailing; Kang, Jie; Chu, Haibin; Zhang, Haixia; Zhao, Yongliang] Inner Mongolia Univ, Coll Chem & Chem Engn, Hohhot 010021, Peoples R China; [Zhao, Yanfang] Inner Mongolia Vocat Coll Chem Engn, Hohhot 010070, Peoples R China in 2020, Cited 40. COA of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Metal-enhanced luminescence (MEL) via Ag@SiO2 nanoparticles provides a promising strategy for the superior luminescence of lanthanide complexes. However, because of the delicate structure of the composites of Ag@SiO2 and complexes, it remains a great challenge to achieve the ideal MEL effect. Herein, five types of Ag@SiO2 nanoparticles with distinct core sizes (100 and 46 nm) and varied silica shell thickness (3, 24, 32, 52 and 55 nm) were prepared. Four kinds of lanthanide complexes RE(BA)(3)center dot H2O and RE(pyca)(3)center dot 2H(2)O (RE = Eu and Tb, BA = benzoate, pyca = 2-pyrazine carboxylate) were synthesized. A series of REL3-Ag@SiO2 (L = BA(-), pyca(-)) composite nanoparticles were prepared through the interaction of the Ag@SiO2 nanoparticles and the complexes. The adsorption of the complexes on the surface of Ag@SiO2 nanoparticles was confirmed by transmission electron microscope and energy dispersive X-ray spectroscopy. Luminescence property investigation showed that the factors affecting the MEL effect included the excitation and emission wavelength of lanthanide complexes, the kinds of lanthanide ions and organic ligands, as well as the core size and shell thickness of Ag@SiO2. Among these factors, the excitation wavelength of lanthanide complexes and the SiO2 shell thickness were found to play decisive roles. Finally, 25.92 times enhancement in luminescent intensity and 7.4 times increase in luminescence quantum yield can be achieved on Tb(BA)(3)center dot H2O by Ag@SiO2 with core size of 46 nm and shell thickness of 24 nm.

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

Srinivasarao, S; Nandikolla, A; Suresh, A; Van Calster, K; De Voogt, L; Cappoen, D; Ghosh, B; Aggarwal, H; Murugesan, S; Sekhar, KVGC in [Srinivasarao, Singireddi; Nandikolla, Adinarayana; Suresh, Amaroju; Aggarwal, Himanshu; Sekhar, Kondapalli Venkata Gowri Chandra] Birla Inst Technol & Sci, Dept Chem, Hyderabad Campus, Hyderabad 500078, Telangana, India; [Calster, Kevin Van; De Voogt, Linda; Cappoen, Davie] Univ Ghent, Fac Biosci Engn, Dept Green Chem & Technol, Coupure Links 653, B-9000 Ghent, Belgium; [Ghosh, Balaram] Birla Inst Technol & Sci, Dept Pharm, Hyderabad Campus, Hyderabad 500078, Telangana, India; [Murugesan, Sankaranarayanan] Birla Inst Technol & Sci, Dept Pharm, Med Chem Res Lab, Pilani 333031, Rajasthan, India published Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents in 2020, Cited 34. Category: Pyrazines. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyrazinamide is an important first-line drug used in shortening TB therapy. In our current work, a series of novel substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives were designed, synthesized, and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra. Among the tested compounds, five compounds (6a, 6e, 6h, 6j and 6k) from Series-I and one compound (7e) from Series-II exhibited significant activity against Mycobacterium tuberculosis H37Ra with 50% inhibitory concentrations (IC50) ranging from 1.35 to 2.18 mu M. To evaluate the efficacy of these compounds, we examined their IC90 values. Five of the most active compounds were found to be more active with IC(90)s ranging from 3.73 to 4.00 mu M and one compound (6e) showed an IC90 of 40.32 mu M. Moreover, single crystals were developed for 6d, 6f and 6n. In addition, most active compounds were evaluated for their cytotoxicity on HEK-293 (human embryonic kidney) cells. Our results indicate that the compounds are nontoxic to human cells. The molecular interactions of the derivatised conjugates in docking studies reveal their suitability for further development.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Srinivasarao, S; Nandikolla, A; Suresh, A; Van Calster, K; De Voogt, L; Cappoen, D; Ghosh, B; Aggarwal, H; Murugesan, S; Sekhar, KVGC or send Email.

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