Category: Pyrazines

An article Amidation Reaction of Quinoline-3-carboxylic Acids with Tetraalkylthiuram Disulfides under Simple Conditions: A facile Synthesis of Quinoline-3-carboxamides WOS:000577748400001 published article about CROSS-COUPLING REACTIONS; CARBOXYLIC-ACIDS; QUINOLINE; SITE; DERIVATIVES; CARBONYLATION; COMPLEXES; RECEPTOR in [Hu, Jingyan; Ye, Xiefeng; Hao, Shuai; Zhao, Qianrui; Zhao, Mingqin; Wei, Yuewei; Wu, Zhiyong; Ji, Xiaoming] Henan Agr Univ, Flavors & Fragrance Engn & Technol Res Ctr Henan, Coll Tobacco Sci, 95 Wenhua Rd, Zhengzhou 450002, Peoples R China; [Wang, Na] China Tobacco Hubei Ind Co Ltd, Ctr Technol, 1355 Jinshan Rd, Wuhan 430040, Peoples R China in 2020, Cited 46. 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

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogues via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides has been developed. The reaction proceeds efficiently under simple reaction conditions and features the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

SDS of cas: 98-97-5. 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

I found the field of Thermodynamics; Chemistry very interesting. Saw the article Mechanochemical synthesis, characterization and thermal study of new cocrystals of ciprofloxacin with pyrazinoic acid and p-aminobenzoic acid published in 2020. Name: Pyrazine-2-carboxylic acid, Reprint Addresses Caires, F (corresponding author), Sao Paulo State Univ, Inst Chem, UNESP, Araraquara, Brazil.; Caires, F (corresponding author), Sao Paulo State Univ, Sch Sci, UNESP, Bauru, Brazil.. The CAS is 98-97-5. Through research, I have a further understanding and discovery 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.

Welcome to talk about 98-97-5, If you have any questions, you can contact de Almeida, AC; Ferreira, PO; Torquetti, C; Ekawa, B; Carvalho, ACS; dos Santos, EC; Caires, F or send Email.. Name: Pyrazine-2-carboxylic acid

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

An article Novel pyrazine based anti-tubercular agents: Design, synthesis, biological evaluation and in silico studies WOS:000516796900043 published article about MYCOBACTERIUM-TUBERCULOSIS; ANTIMYCOBACTERIAL ACTIVITY; ACID HYDRAZONES; DERIVATIVES; RESISTANCE; DOCKING; DRUGS; GRANULOCYTES; INHIBITORS; PREDICTION in [Hassan, Nayera W.; Saudi, Manal N.; Abdel-Ghany, Yasser S.; Ismail, Azza; Elzahhar, Perihan A.; El-Hawash, Soad A.] Alexandria Univ, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21521, Egypt; [Sriram, Dharmarajan] Birla Inst Technol & Sci Pilani, Med Chem & Drug Discovery Res Lab, Pharm Grp, Hyderabad Campus, Jawahar Nagar 500078, Telangana, India; [Nassra, Rasha] Alexandria Univ, Fac Med, Dept Med Biochem, Alexandria, Egypt; [Abdel-Aziz, Marwa M.] Al Azhar Univ, Reg Ctr Mycol & Biotechnol, Cairo 11759, Egypt in 2020, Cited 84. 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

TB continues to be a leading health threat despite the availability of powerful anti-TB drugs. We report herein the design and synthesis of various hybrid molecules comprising pyrazine scaffold and various formerly identified anti-mycobacterial moieties. Thirty-one compounds were screened in vitro for their activity against Mycobacterium tuberculosis H37Rv strain using MABA assay. The results revealed that six compounds (8a, 8b, 8c, 8d, 14b and 18) displayed significant activity against Mtb with MIC values <= 6.25 mu g/ml versus 6.25 mu g/ml for pyrazinamide. The most active compounds were then assessed for their in vitro cytotoxicity against PBMC normal cell line using MTT assay and showed SI > 200. Several in silico studies have been carried out for target fishing of the novel compounds such as shape-based similarity, pharmacophore mapping and inverse docking. Based on this multi-step target fishing study, we suggest that pantothenate synthetase could be the possible target responsible for the action of these compounds. The most active compounds were then successfully docked into the active site of pantothenate synthetase enzyme with favorable binding interactions. In addition, in silico prediction of physicochemical, ADMET and drug-like properties were also determined indicating that compounds 8b, 8c and 8d are promising candidates for the development of new anti-TB agents with enhanced activity and better safety profile.

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

Formula: C5H4N2O2. Authors Swiderski, G; Kalinowska, M; Jablonska-Trypuc, A; Wolejko, E; Wydro, U; Lyszczek, R; Rusinek, I; Lewandowski, W in ELSEVIER published article about in [Swiderski, Grzegorz; Kalinowska, Monika; Jablonska-Trypuc, Agata; Wolejko, Elzbieta; Wydro, Urszula; Lewandowski, Wlodzimierz] Bialystok Tech Univ, Dept Chem Biol & Biotechnol, Wiejska 45E St, PL-15351 Bialystok, Poland; [Lyszczek, Renata; Rusinek, Iwona] UMCS, Dept Gen & Coordinat Chem, MC Sklodowska Sq 2, PL-20031 Lublin, Poland in 2021, Cited 50. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Diazinecarboxylic acids (pyridazine-3-carboxylic, pyridazine-4-carboxylic, pyrimidine-2-carboxylic, pyrimidine-4-carboxylic, pyrimidine-5-carboxylic and pyrazine-2-carboxylic acids) were characterized by means of spectroscopic (FT-Raman, FTIR, UV, (HNMR)-H-1, (CNMR)-C-13) and thermogravimetric analysis as well as antimicrobial and cytotoxic tests. The structures of diazinecarboxylic acids were calculated by the DFT method (B3LYP/6-311G(d, p). For the most stable conformers, the energy of HOMO and LUMO molecular orbitals, the geometric (HOMA, GEO, EN, I6) and magnetic (NICS) aromaticity indices, NBO electronic charge distribution, sEDA and pEDA indexes, Wiberg Bond Order, Wiberg Index and theoretical IR and NMR spectra have been calculated. The energies of protonating and deprotonating acids were also calculated. The effect of the nitrogen heteroatom position in the aromatic ring in relation to the position of the carboxyl group on the electronic charge distribution, thermal stability, antimicrobial and cytotoxicity activities of the examined acids was determined. Antimicrobial activity of tested acids against of Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosaand Candida albicanswas calculated based on MTT colorimetric assay (MCA). The cytotocic effect of diazynecarboxylic acids was examined in A375 melanoma cell line and DLD-1 cell line. A biplot analysis was performed in order to determine the correlations between selected parameters of the tested compounds and relative cell viability of E. coli, B. subtilis, P. aeruginosa, C. albicans, A375 and DLD-1 cell lines. Thermal behaviour of all investigated carboxylic acids was investigated using thermogravimetry (TG) and differential scanning calorimetry (DSC) techniques in flowing air atmosphere. All compounds are stable in room temperature. (C) 2021 Elsevier B.V. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Swiderski, G; Kalinowska, M; Jablonska-Trypuc, A; Wolejko, E; Wydro, U; Lyszczek, R; Rusinek, I; Lewandowski, W or send Email.. Formula: C5H4N2O2

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

In 2020 CHEM BIOL DRUG DES published article about CYSTEINE PROTEASE; TRYPANOSOMA-CRUZI; DRUG DISCOVERY; INTEGRATION; ISOFORMS; LIGANDS; IMPROVE in [de Albuquerque, Sergio; Duque, Carla; da Silva, Joao Santana] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Sao Paulo, Brazil; [Cianni, Lorenzo; de Vita, Daniela; Leitao, Andrei; Montanari, Carlos A.; Ribeiro, Jean F. R.] Univ Sao Paulo, Inst Quim Sao Carlos, Grp Quim Med, Ave Trabalhador Sancarlense 400, BR-13566590 Sao Carlos, SP, Brazil; [Gomes, Ana S. M.; Gomes, Paula; Teixeira, Catia] Univ Porto, Dept Quim & Bioquim, LAQV REQUIMTE, Fac Ciencias, Porto, Portugal; [Laughton, Charles] Univ Nottingham, Sch Pharm, Nottingham, England; [Laughton, Charles] Univ Nottingham, Ctr Biomol Sci, Nottingham, England; [Montanari, Raphael] Univ Sao Paulo, Ctr Robot Sao Carlos, EESC ICMC, Sao Paulo, Brazil; [Ribeiro, Jean F. R.] Univ Fed Goias, Inst Trop Pathol & Publ Hlth, Goiania, Go, Brazil in 2020, Cited 59. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Computed Properties of C5H4N2O2

Cruzain is an established target for the identification of novel trypanocidal agents, but how good are in vitro/in vivo correlations? This work describes the development of a random forests model for the prediction of the bioavailability of cruzain inhibitors that areTrypanosoma cruzikillers. Some common properties that characterize drug-likeness are poorly represented in many established cruzain inhibitors. This correlates with the evidence that many high-affinity cruzain inhibitors are not trypanocidal agents againstT. cruzi. On the other hand,T. cruzikillers that present typical drug-like characteristics are likely to show better trypanocidal action than those without such features. The random forests model was not outperformed by other machine learning methods (such as artificial neural networks and support vector machines), and it was validated with the synthesis of two new trypanocidal agents. Specifically, we report a new lead compound,Neq0565, which was tested onT. cruziTulahuen (beta-galactosidase) with a pEC(50)of 4.9. It is inactive in the host cell line showing a selectivity index (SI = EC50cyto/EC50T. cruzi) higher than 50.

Computed Properties of C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact de Albuquerque, S; Cianni, L; de Vita, D; Duque, C; Gomes, ASM; Gomes, P; Laughton, C; Leitao, A; Montanari, CA; Montanari, R; Ribeiro, JFR; da Silva, JS; Teixeira, C or send Email.

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

Gopal, P; Sarathy, JP; Yee, M; Ragunathan, P; Shin, J; Bhushan, S; Zhu, JH; Akopian, T; Kandror, O; Lim, TK; Gengenbacher, M; Lin, QS; Rubin, EJ; Gruber, G; Dick, T in [Gopal, Pooja; Sarathy, Jickky Palmae] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Med, Singapore, Singapore; [Yee, Michelle; Dick, Thomas] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Microbiol & Immunol, Singapore, Singapore; [Ragunathan, Priya; Shin, Joon; Bhushan, Shashi; Grueber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore, Singapore; [Zhu, Junhao; Akopian, Tatos; Kandror, Olga; Rubin, Eric J.] Harvard Univ, Harvard TH Chan Sch Publ Hlth, Dept Immunol & Infect Dis, Boston, MA 02115 USA; [Lim, Teck Kwang; Lin, Qingsong] Natl Univ Singapore, Dept Biol Sci, Singapore, Singapore; [Gengenbacher, Martin; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Gengenbacher, Martin; Dick, Thomas] Seton Hall Univ, Dept Med Sci, Hackensack Meridian Med Sch, Nutley, NJ 07110 USA; [Gopal, Pooja] Merck Res Labs, MSD Translat Med Res Ctr, Singapore, Singapore published Pyrazinamide triggers degradation of its target aspartate decarboxylase in 2020, Cited 29. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyrazinamide is a sterilizing first-line tuberculosis drug. Genetic, metabolomic and biophysical analyses previously demonstrated that pyrazinoic acid, the bioactive form of the prodrug pyrazinamide (PZA), interrupts biosynthesis of coenzyme A in Mycobacterium tuberculosis by binding to aspartate decarboxylase PanD. While most drugs act by inhibiting protein function upon target binding, we find here that pyrazinoic acid is only a weak enzyme inhibitor. We show that binding of pyrazinoic acid to PanD triggers degradation of the protein by the caseinolytic protease ClpC1-ClpP. Thus, the old tuberculosis drug pyrazinamide exerts anti-bacterial activity by acting as a target degrader, a mechanism of action that has recently emerged as a successful strategy in drug discovery across disease indications. Our findings provide the basis for the rational discovery of next generation PZA.

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

An article Complementary Features of Inorganic (M-X) and Organic (C-X ‘) Halogens in C-X ‘center dot center dot center dot X-M Halogen Bonds: A Study Based on Structure, Energy, and Topological Electron Density WOS:000526390000016 published article about HALIDE ION SYNTHON; CRYSTAL-STRUCTURES; INTERMOLECULAR INTERACTIONS; HYDROGEN-BONDS; MOLECULES; HIERARCHY; CROSSOVER; LIGANDS; METALS; BR in [Khavasi, Hamid Reza; Gholami, Akram; Hosseini, Mahdieh; Nikpoor, Leyla] Shahid Beheshti Univ, Dept Inorgan Chem & Catalysis, Tehran 1983963113, Iran; [Eskandari, Kiamars] Isfahan Univ Technol, Dept Chem, Esfahan 8415683111, Iran in 2020, Cited 45. 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

A family of 10 compounds, each containing a MX2-pyrazine carboxylate complex anion and a protonated halo- (X’-) amino pyridine cation (MX2 = ZnCl2, ZnBr2, ZnI2, HgBr2, and HgI2; X’ = Cl, Br, I), are presented; a suitable system for pursuing C-X’center dot center dot center dot X-M halogen bonding (XB). The influence of halogen manipulation, metal ion and coordination variation on the nature and strength of C-X’center dot center dot center dot X-M interactions was discussed in terms of geometrical parameters, binding energies and charge density analysis with emphasis on the Laplacian of the electron density, del(2)rho. Interplay of XBs with other noncovalent interactions, mainly N-H center dot center dot center dot XM and N-py-H+center dot center dot center dot O- bonds, in supramolecular assemblies, were also investigated. The C-X’center dot center dot center dot X-M and N-H center dot center dot center dot X-M bonds have rationally been modified in strength upon changing the halogens involved, leading to systematic variations in the crystal packing.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Khavasi, HR; Gholami, A; Hosseini, M; Nikpoor, L; Eskandari, K or send Email.

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

Authors Hu, JY; Ye, XF; Hao, S; Zhao, QR; Zhao, MQ; Wei, YW; Wu, ZY; Wang, N; Ji, XM in WILEY-V C H VERLAG GMBH published article about CROSS-COUPLING REACTIONS; CARBOXYLIC-ACIDS; QUINOLINE; SITE; DERIVATIVES; CARBONYLATION; COMPLEXES; RECEPTOR in [Hu, Jingyan; Ye, Xiefeng; Hao, Shuai; Zhao, Qianrui; Zhao, Mingqin; Wei, Yuewei; Wu, Zhiyong; Ji, Xiaoming] Henan Agr Univ, Flavors & Fragrance Engn & Technol Res Ctr Henan, Coll Tobacco Sci, 95 Wenhua Rd, Zhengzhou 450002, Peoples R China; [Wang, Na] China Tobacco Hubei Ind Co Ltd, Ctr Technol, 1355 Jinshan Rd, Wuhan 430040, Peoples R China in 2020, Cited 46. HPLC of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogues via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides has been developed. The reaction proceeds efficiently under simple reaction conditions and features the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

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.. HPLC of Formula: C5H4N2O2

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

Product Details of 98-97-5. Recently I am researching about SIGNALING PATHWAY; NATURAL-PRODUCTS; DERIVATIVES; APOPTOSIS; DESIGN; DISCOVERY; PREDICTION; CURCUMIN; ACID, Saw an article supported by the national major science and technology special project for significant new drugs development [2018ZX09711001-005-018]; medical and health science and technology innovation project of Chinese Academy of Medical Science [2017-I2M-3-021/2019-I2M-1-005]; Tianjin special support program for talent development [TJTZJH-GCCCXCYTD-1-30]. Published in MDPI in BASEL ,Authors: Wang, JW; Hong, G; Li, GL; Wang, WZ; Liu, TJ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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.

Product Details of 98-97-5. 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 2020 ACS OMEGA published article about GOLD COMPLEXES; GOLD(III) COMPLEXES; AU(I) COMPLEXES; ACID; AURANOFIN; LIGANDS; AGENTS; BROAD in [Stenger-Smith, Jenny; Chakraborty, Indranil; Ouattara, Ramatoulaye; Mascharak, Pradip K.] Univ Calif Santa Cruz, Dept Chem & Biochem, Santa Cruz, CA 95064 USA; [Kamariza, Mireille; Bertozzi, Carolyn R.] Stanford Univ, Dept Chem, Stanford, CA 94305 USA in 2020, Cited 42. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Category: Pyrazines

As part of the quest for new gold drugs, we have explored the efficacy of three gold complexes derived from the tuberculosis drug pyrazinamide (PZA), namely, the gold(I) complex [Au(PPh3)(PZA)]OTf (1, OTf = trifluoromethanesulfonate) and two gold(III) complexes [Au(PZA)Cl-2] (2) and [Au(PZO)Cl-2] (3, PZO = pyrazinoic acid, the metabolic product of PZA) against two mycobacteria, Mycobacterium tuberculosis and Mycobacterium smegmatis. Only complex 1 with the {Au(PPh3)}(+) moiety exhibits significant bactericidal activity against both strains. In the presence of thiols, 1 gives rise to free PZA and {Au(PPh3)}-thiol polymeric species. A combination of PZA and the {Au(PPh3)}-thiol polymeric species appears to lead to enhanced efficacy of 1 against M. tuberculosis.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Stenger-Smith, J; Kamariza, M; Chakraborty, I; Ouattara, R; Bertozzi, CR; Mascharak, PK or send Email.

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