Month: November 2021

Samie, A; Salimi, A in [Samie, Ali; Salimi, Alireza] Ferdowsi Univ Mashhad, Fac Sci, Dept Chem, Mashhad, Razavi Khorasan, Iran published Orientation-dependent conformational polymorphs in two similar pyridine/pyrazine phenolic esters in 2019, Cited 67. Category: Pyrazines. 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.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Samie, A; Salimi, A or send Email.

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

In 2020 BIOORG MED CHEM LETT published article about ANTI-TUBERCULAR ACTIVITY; DESIGN; HYBRIDS; 1,2,3-TRIAZOLE; HYBRIDIZATION; ANTIMYCOBACTERIAL; DIARYLQUINOLINE in [Reddyrajula, Rajkumar; Dalimba, Udayakumar] Natl Inst Technol Karnataka, Dept Chem, Organ Chem Lab, Mangalore 575025, India in 2020, Cited 38. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Application In Synthesis of Pyrazine-2-carboxylic acid

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.

Application In Synthesis of Pyrazine-2-carboxylic acid. 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

An article Pyrazinamide triggers degradation of its target aspartate decarboxylase WOS:000564272800001 published article about TUBERCULOSIS; RESISTANCE; MUTATIONS; PROTEASE; COMPLEX 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 in 2020, Cited 29. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Category: Pyrazines

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.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact 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 or send Email.

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

In 2020 NAT COMMUN published article about TUBERCULOSIS; RESISTANCE; MUTATIONS; PROTEASE; COMPLEX 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 in 2020, Cited 29. 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

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.

Recommanded Product: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact 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 or send Email.

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

Name: Pyrazine-2-carboxylic acid. In 2019 J AM CHEM SOC published article about TERTIARY BORONIC ESTERS; AMINOBORONIC ACID-DERIVATIVES; ASYMMETRIC HYDROBORATION; PINACOLBORYL ADDITION; AMINOBORATION; ALKENES; SECONDARY; HYDROFUNCTIONALIZATION; HYDROALKYNYLATION; BORYLATION in [Bai, Xiao-Yan; Zhao, Wei; Sun, Xin; Li, Bi-Jie] Tsinghua Univ, Dept Chem, CBMS, Beijing 100084, Peoples R China in 2019, Cited 89. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Chiral alpha- and beta-aminoboronic acids exhibit unique biological activities. General methods for the synthesis of these bioisosteres of amino acids are highly desirable. We report a facile preparation of these compounds through rhodium-catalyzed regiodivergent and enantioselective hydroboration of enamides. Catalytic asymmetric synthesis of alpha- and beta-aminoboronic esters with high regio-, diastereo-, and enantioselectivities were achieved through effective catalyst control and tuning substrate geometry. Starting from easily available materials, this strategy provides a unified synthetic access to both enantioenriched alpha-boration and beta-boration products. The synthetic utility of these methods was demonstrated by efficient synthesis of an anticancer drug molecule and diverse transformations of the boration products.

Name: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Bai, XY; Zhao, W; Sun, X; Li, BJ or send Email.

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

Category: Pyrazines. 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.

Category: Pyrazines. 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.

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

Computed Properties of C5H4N2O2. Authors Sahoo, T; Sarkar, S; Ghosh, SC in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Sahoo, Tapan; Sarkar, Souvik; Ghosh, Subhash Chandra] Cent Salt & Marine Chem Res Inst CSIR CSMCRI, Nat Prod & Green Chem Div, GB Marg, Bhavnagar 364002, Gujarat, India; [Sahoo, Tapan; Ghosh, Subhash Chandra] Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India in 2021, Cited 50. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A simple and facile copper(II) mediated protocol for C-8 amination of 1-naphthylamide derivatives is reported here. Picolinamide and its derivatives were used as a bidentate directing group for the C-8 amination reaction. Various substituted naphthylamide derivatives with numerous cyclic and acyclic amines proceed in good yields under mild conditions. Air was used solely as an oxidant. (C) 2021 Elsevier Ltd. All rights reserved.

Computed Properties of C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Sahoo, T; Sarkar, S; Ghosh, SC or send Email.

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

In 2019 EUR J MED CHEM published article about BIOLOGICAL EVALUATION; MOLECULAR DOCKING; 20S PROTEASOME; DESIGN; DERIVATIVES; IDENTIFICATION; DEGRADATION; GENERATION; APOPTOSIS; MYELOMA in [Dong, Xiao-Wu; Zhang, Jian-Kang; Che, Jin-Xin; Liu, Tao; Hu, Yong-Zhou] Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Zhejiang Prov Key Lab Anticanc Drug Res, Hangzhou Inst Innovat Med,Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; [Xu, Lei; Hu, Xiao-Bei; Sheng, Li; Gao, An-Hui; Li, Jia; Liu, Tao; Zhou, Yu-Bo] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; [Xu, Lei; Hu, Xiao-Bei; Sheng, Li; Gao, An-Hui; Li, Jia; Zhou, Yu-Bo] Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; [Zhang, Jian-Kang] Zhejiang Univ City Coll, Sch Med, Hangzhou 310015, Zhejiang, Peoples R China; [Cheng, Gang] Zhejiang Chinese Med Univ, Coll Pharmaceut Sci, Hangzhou 311402, Zhejiang, Peoples R China in 2019, Cited 33. 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

The potential of specific proteasome inhibitors to act as anti-cancer agents has attracted intensive investigations. The proteasome can be covalently inhibited by epoxyketone derivatives via a two-step reaction. Several computational approaches have been developed to mimic the covalent binding event. Compound 1 composed of a six-membered heterocyclic ring was designed by using covalent docking. With a possible different binding mode from the clinical compound Carfilzomib, it occupied the 55 pocket of 20S proteasome and showed favorable inhibitory activity. Subsequently optimization and evaluation were taken place. Among these compounds, 11h demonstrated extraordinary in vitro inhibitory activity and selectivity, and good in vivo proteasome inhibitory activity, a favorable pharmacokinetic profile and xenograft tumor inhibition. The possible binding pattern of compound 11h against proteasome was further fully explored via calculations, providing a theoretical basis for finding potent proteasome inhibitors. (C) 2018 Elsevier Masson SAS. All rights reserved.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Dong, XW; Zhang, JK; Xu, L; Che, JX; Cheng, G; Hu, XB; Sheng, L; Gao, AH; Li, J; Liu, T; Hu, YZ; Zhou, YB or send Email.

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

An article Identification of Substituted Amino Acid Hydrazides as Novel Anti-Tubercular Agents, Using a Scaffold Hopping Approach WOS:000539293400120 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. HPLC of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 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.

HPLC of Formula: C5H4N2O2. 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.

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

Authors Zhang, ZG; Hao, K; Li, HW; Lu, R; Liu, CX; Zhou, MZ; Li, BY; Meng, ZB; Hu, QH; Jiang, C in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about MECHANISMS; IDENTIFICATION; INFLAMMASOME; CHEMOTAXIS in [Zhang, Zhenguo; Lu, Ran; Jiang, Cheng] China Pharmaceut Univ, Jiang Su Key Lab Drug Design & Optimizat, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Zhang, Zhenguo; Lu, Ran; Li, Baiyang; Meng, Zibo; Jiang, Cheng] China Pharmaceut Univ, Dept Med Chem, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Hao, Kun] China Pharmaceut Univ, State Key Lab Nat Med, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Li, Hanwen; Liu, Chunxiao; Zhou, Mengze; Hu, Qinghua] China Pharmaceut Univ, Key Lab Drug Metab & Pharmacokinet, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China in 2019, Cited 35. COA of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The P2Y(14) receptor (P2Y(14)R) plays a key role in the modulation of inflammatory process, but very few classes of antagonists have been reported. A series of 3-amide benzoic acid derivatives were identified as novel and potent P2Y(14)R antagonists. The most potent antagonist, 16c, showed comparable activity (IC50 = 1.77 nM) to PPTN, the most potent P2Y(14)R antagonist reported. Compound 16c demonstrated dramatically improved aqueous solubility and excellent metabolic stability in rat and human microsomes. Investigation of the anti-inflammatory effect of 16c was performed in MSU treated THP-1 cells by flow cytometry, Western Blot and immunofluorescence labeling technology, which exhibited that 16c might be a promising candidate for further research. (C) 2019 Elsevier Masson SAS. All rights reserved.

COA of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Zhang, ZG; Hao, K; Li, HW; Lu, R; Liu, CX; Zhou, MZ; Li, BY; Meng, ZB; Hu, QH; Jiang, C or send Email.

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