Category: 98-97-5

An article N-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)picolinamide as a new inhibitor of mitochondrial complex III: Synthesis, biological evaluation and computational simulations WOS:000546629300011 published article about CYTOCHROME BC(1) COMPLEX; IRON-SULFUR PROTEIN; BC1 COMPLEX; DISCOVERY; SITE; FUNGICIDE; AMETOCTRADIN; RESISTANCE; MECHANISM; BINDING in [Cheng, Hua; Yang, Lu; Liu, Hong-Fu; Zhang, Rui] Hubei Univ Arts & Sci, Dept Chem Engn & Food Sci, Xiangyang 441053, Peoples R China; [Chen, Cheng] Wuhan Univ Technol, State Key Lab Adv Technol Mat Synth & Proc, Wuhan 430070, Peoples R China; [Wu, Yuan; Jiang, Wen] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China in 2020, Cited 47. 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

Mitochondrial complex III is one of the most promising targets for a number of pharmaceuticals and fungicides. Due to the wide-spread use of complex III-inhibiting fungicides, a considerable increase of resistance has occurred worldwide. Therefore, inhibitors with novel scaffolds and potent activity against complex III are still in great demand. In this article, a new series of amide compounds bearing the diaryl ether scaffold were designed and prepared, followed by the biological evaluation. Gratifyingly, several compounds demonstrated potent activity against succinate-cytochrome c reductase (SCR, a mixture of mitochondrial complex II and complex III), with compound 3w possessing the best inhibitory activity (IC50 = 0.91 +/- 0.09 mu mol/L). Additional studies verified that 3w was a new inhibitor of complex III. Moreover, computational simulations elucidated that 3w should bind to the Q(o) site of complex III. We believe this work will be valuable for the preparation and discovery of more complex III inhibitors.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Cheng, H; Yang, L; Liu, HF; Zhang, R; Chen, C; Wu, Y; Jiang, W or concate me.. SDS of cas: 98-97-5

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

Computed Properties of C5H4N2O2. Authors Alsayed, SSR; Lun, SC; Payne, A; Bishai, WR; Gunosewoyo, H in WILEY published article about in [Alsayed, Shahinda S. R.; Gunosewoyo, Hendra] Curtin Univ, Fac Hlth Sci, Sch Pharm & Biomed Sci, Perth, WA, Australia; [Lun, Shichun; Bishai, William R.] Johns Hopkins Sch Med, Dept Med, Ctr TB Res, Div Infect Dis, Baltimore, MD 21205 USA; [Payne, Alan] Curtin Univ, Sch Mol & Life Sci, Perth, WA, Australia; [Bishai, William R.] Howard Hughes Med Inst, Chevy Chase, MD USA in 2021, Cited 54. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Several rationally designed isoniazid (INH), pyrazinamide (PZA) and ciprofloxacin (CPF) derivatives were conveniently synthesized and evaluated in vitro against H37Rv Mycobacterium tuberculosis (M. tb) strain. CPF derivative 16 displayed a modest activity (MIC = 16 mu g/ml) and was docked into the M. tb DNA gyrase. Isoniazid-pyrazinoic acid (INH-POA) hybrid 21a showed the highest potency in our study (MIC = 2 mu g/ml). It also retained its high activity against the other tested M. tb drug-sensitive strain (DS) V4207 (MIC = 4 mu g/ml) and demonstrated negligible cytotoxicity against Vero cells (IC50 >= 64 mu g/ml). Four tested drug-resistant (DR) M. tb strains were refractory to 21a, similar to INH, whilst being sensitive to CPF. Compound 21a was also inactive against two non-tuberculous mycobacterial (NTM) strains, suggesting its selective activity against M. tb. The noteworthy activity of 21a against DS strains and its low cytotoxicity highlights its potential to treat DS M. tb.

Computed Properties of C5H4N2O2. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Alsayed, SSR; Lun, SC; Payne, A; Bishai, WR; Gunosewoyo, H or concate me.

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

An article Cu(II)-Mediated N-H and N-Alkyl Aryl Amination and Olefin Aziridination WOS:000461843900081 published article about C-H; STEREOSPECIFIC SYNTHESIS; ELECTROPHILIC AMINATION; CATALYZED AMINATION; BONDS in [Munnuri, Sailu; Anugu, Raghunath Reddy; Falck, John R.] Univ Texas Southwestern Med Ctr Dallas, Dept Biochem, Div Chem, Dallas, TX 75390 USA in 2019, Cited 32. Safety 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

Cu(II)-mediated direct NH2 and NH alkyl aryl aminations and olefin aziridinations are described. These room temperature, one-pot, environmentally friendly procedures replace costly Rh-2 catalysts and, in some instances, display important differences with comparable Rh-2- and Fe-supported reactions.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Munnuri, S; Anugu, RR; Falck, JR or concate me.. Application In Synthesis of Pyrazine-2-carboxylic acid

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

Quality Control 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.

Quality Control of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, 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 concate me.

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

Authors Yang, ZF; Yang, XD; Jin, LY; Dong, KL; Ma, PT; Niu, JY; Wang, JP in TAYLOR & FRANCIS LTD published article about COMPLEXES; AZIDO; MN in [Yang, Zongfei; Yang, Xindi; Jin, Linyu; Dong, Kaili; Ma, Pengtao; Niu, Jingyang; Wang, Jingping] Henan Univ, Henan Key Lab Polyoxometalate Chem, Inst Mol & Crystal Engn, Coll Chem & Chem Engn, Kaifeng 475004, Henan, Peoples R China in 2020, Cited 29. Safety 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 high-nuclearity nickel-substituted polyoxotungstate, Na6K5.5H4.5{[Ni-8(OH)(6)(H2O)(2)](CO3)(3)(SiW9O34)(2)}center dot 22H(2)O (1), has been obtained by the reaction of Na-10[alpha-SiW9O34]center dot 18H(2)O, Ni(NO3)(2)center dot 6H(2)O and K(2)CO(3)in aqueous solution and characterized by IR spectroscopy, single crystal X-ray diffraction, thermal gravimetric analysis and elemental analysis. Carbonate is not only used to adjust the pH of the solution, but also is a structure-stabilizing agent. The polyoxoanion {[Ni-8(OH)(6)(H2O)(2)](CO3)(3)(SiW9O34)(2)}(16-)(1a) can be regarded as two {[Ni-4(OH)(3)(H2O)](SiW9O34)} subunits connected by three carbonate groups, which represents the first polyanion containing an octanuclear nickel cluster based on trivacant Keggin-type polyoxotungstate {XW9} (X = heteroatom). The subunit {[Ni-4(OH)(3)(H2O)](SiW9O34)} can be viewed as a tetranuclear nickel cluster linked to a trivacant Keggin-type polyoxotungstate {SiW9O34}. Furthermore, magnetic measurements show that1exhibits antiferromagnetic interactions.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Yang, ZF; Yang, XD; Jin, LY; Dong, KL; Ma, PT; Niu, JY; Wang, JP or concate me.. Product Details of 98-97-5

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

Jiang, YQ; He, L; Green, J; Blevins, H; Guo, CQ; Patel, SH; Halquist, MS; Mcrae, M; Venitz, J; Wang, XY; Zhang, SJ 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 published Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization in 2019, Cited 30. Quality Control 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.

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.

Quality Control of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, 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 concate me.

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

Application In Synthesis of Pyrazine-2-carboxylic acid. I found the field of Food Science & Technology very interesting. Saw the article Alkylpyrazines from Coffee are Extensively Metabolized to Pyrazine Carboxylic Acids in the Human Body published in 2019, Reprint Addresses Richling, E (corresponding author), Tech Univ Kaiserslautern, Dept Chem, Div Food Chem & Toxicol, Erwin Schrodinger Str 52, D-67663 Kaiserslautern, Germany.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

Scope Coffee is a complex mixture of over 1000 compounds, including diverse heteroaromatic compounds such as alkylpyrazines. Little is known about the intake, metabolism, and bodily distribution of these compounds. Therefore, a human intervention study is conducted to investigate the excretion of alkylpyrazine metabolites in urine after the ingestion of brewed coffee containing alkylpyrazines. Methods and results After consuming a diet without heat-processed food, ten volunteers consumed 500 mL of freshly brewed coffee prepared from coffee pads, providing intakes of 2-methylpyrazine (2-MeP), 2,5-dimethylpyrazine (2,5-DMeP), and 2,6-dimethylpyrazine (2,6-DMeP) amounting to 17.2, 4.4, and 4.9 mu mol, respectively. These alkylpyrazines are metabolized into the corresponding pyrazine carboxylic acids, namely pyrazine-2-carboxylic acid (PA), 5-hydroxypyrazine-2-carboxylic acid (5-OHPA), 5-methylpyrazine-2-carboxylic acid (5-MePA), and 6-methylpyrazine-2-carboxylic acid (6-MePA). In total, 64% of the ingested 2-MeP is excreted as PA, as well as 26% as 5-OHPA, while 91% and 97% of the ingested 2,5-DMeP and 2,6-DMeP are recovered as 5-MePA and 6-MePA, respectively, in urine samples collected after coffee consumption. Conclusion This study provides evidence that alkylpyrazines are rapidly metabolized into the corresponding carboxylic acids and excreted via urine by humans, which is consistent with earlier rodent studies.

Application In Synthesis of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Kremer, JI; Pickard, S; Stadlmair, LF; Glass-Theis, A; Buckel, L; Bakuradze, T; Eisenbrand, G; Richling, E or concate me.

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

Computed Properties of C5H4N2O2. 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.

Computed Properties of C5H4N2O2. About Pyrazine-2-carboxylic acid, 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 concate me.

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

Recommanded Product: 98-97-5. 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.

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.

Recommanded Product: 98-97-5. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Stenger-Smith, J; Kamariza, M; Chakraborty, I; Ouattara, R; Bertozzi, CR; Mascharak, PK or concate me.

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

Tudos, M; Anghel, EM; Culita, DC; Somacescu, S; Calderon-Moreno, J; Tecuceanu, V; Dumitrascu, FD; Dracea, O; Popa, M; Marutescu, L; Bleotu, C; Curutiu, C; Chifiriuc, MC in [Tudos, Madalina; Anghel, Elena Maria; Culita, Daniela C.; Somacescu, Simona; Calderon-Moreno, Jose] Ilie Murgulescu Inst Phys Chem, 202 Splaiul Independentei, Bucharest 060021, Romania; [Tecuceanu, Victorita; Dumitrascu, Florea D.] Ctr Organ Chem, 202A Spiaiul Independentei, Bucharest 060023, Romania; [Dracea, Olguta] Cantacussino Natl Inst Res Microbiol & Immunol, 103 Splaiul Independentei, Bucharest 050096, Romania; [Popa, Marcela; Marutescu, Luminita; Curutiu, Carmen; Chifiriuc, Mariana C.] Univ Bucharest, Microbiol Immunol Dept, Fac Biol, Aleea Portocalelor 1-3, Bucharest 060101, Romania; [Popa, Marcela; Marutescu, Luminita; Chifiriuc, Mariana C.] Univ Bucharest ICUB, Res Inst, Bvd M Kogalniceanu 36-46, Bucharest 50107, Romania; [Bleotu, Coralia] Stefan S Nicolau Virol Inst, Mihai Bravu 285, Bucharest 030317, Romania published Covalent coupling of tuberculostatic agents and graphene oxide: A promising approach for enhancing and extending their antimicrobial applications in 2019, Cited 57. Computed Properties of C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

In this work, we present a simple, two-stage method for the preparation of new and efficient antimicrobial hybrid systems, based on isoniazid and pyrazine-2-carbohydrazide tuberculostatic agents covalently linked to graphene oxide. In the first step, the carboxyl groups of graphene oxide are activated by transforming them into the corresponding acid chloride groups, which, in the second step, will react with the amino groups of the two drugs. Pyrazine-2-carbohydrazide was obtained from pyrazinoic acid and hydrazine hydrate and was confirmed by nuclear magnetic resonance spectroscopy. The materials have been characterized by elemental analysis, infrared spectroscopy, Raman spectroscopy, scanning electron microscopy, and X-ray photoelectron spectroscopy. Their antimicrobial activity was tested on mycobacterial (Mycobacterium terrae), as well as on Gram-negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853), Gram-positive bacteria (Staphylococcus aureus ATCC 6538, Staphylococcus aureus ATCC 25923) and fungal (Candida albicans ATCC 10231), in planktonic and biofilm growth state. The biocompatibility of the tested compounds was assessed in vitro by live-dead fluorescence staining and flow cytometry. The results of this study have shown that the functionalization of graphene oxide with isoniazid and pyrazine-2-carbohydrazide both enhanced the anti-mycobacterial activity of the respective drugs and extended their antimicrobial spectrum towards other microbial strains, in planktonic and biofilm growth state, showing a promising potential for mitigating the impact of antimicrobial resistance and the deleterious effects of microbial biofilms. At the active tuberculostatic concentrations, the tested compounds exhibit very low cytotoxicity and do not interfere with the cellular cycle of Hep-2 cells. The flow cytometry and live/dead fluorescence staining proved that the tested compounds exhibit a microbicidal effect through induction of cellular lesions, consecutive to membrane depolarization.

Computed Properties of C5H4N2O2. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Tudos, M; Anghel, EM; Culita, DC; Somacescu, S; Calderon-Moreno, J; Tecuceanu, V; Dumitrascu, FD; Dracea, O; Popa, M; Marutescu, L; Bleotu, C; Curutiu, C; Chifiriuc, MC or concate me.

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