Pyrazines

Authors Zhao, FY; Sun, X; Lu, W; Xu, L; Shi, JZ; Yang, SL; Zhou, MY; Su, F; Lin, F; Cao, FL in TAYLOR & FRANCIS LTD published article about ANTITUMOR-ACTIVITY; QUINOXALINE DERIVATIVES; THIOPHENE DERIVATIVES; CRYSTAL-STRUCTURE; TUMOR-CELLS; ANTICANCER; CYTOTOXICITY; COPPER(II); INHIBITORS; COMPLEXES in [Zhao, Fengyi; Xu, Li; Cao, Fuliang] Nanjing Forestry Univ, Coinnovat Ctr Sustainable Forestry Southern China, Nanjing 210037, Peoples R China; [Zhao, Fengyi; Cao, Fuliang] Nanjing Forestry Univ, Coll Forestry, Nanjing, Peoples R China; [Zhao, Fengyi; Sun, Xu; Lu, Wen; Xu, Li; Shi, Jiuzhou] Nanjing Forestry Univ, Coll Sci, Nanjing, Peoples R China; [Sun, Xu] Nanjing Forestry Univ, Coll Informat Sci & Technol, Nanjing, Peoples R China; [Yang, Shilong; Zhou, Mengyi; Su, Fan; Lin, Feng] Nanjing Forestry Univ, Adv Anal & Testing Ctr, Nanjing, Peoples R China in 2020, Cited 60. 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

Several dehydroabietylamine derivatives containing heterocyclic moieties such as thiophene and pyrazine ring were successfully synthesized. The antiproliferative activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides were investigated in vitro against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver), and HUVEC (umbilical vein) cells by MTT assay. The toxicity of L-1-L-10 (IC50 = 5.92- >100 mu M) was lower than L-0 (1.27 mu M) and DOX (4.40 mu M) in every case. Compound L-1 had higher anti-HepG2 (0.66 mu M), anti-MCF-7 (5.33 mu M), and anti-A549 (2.11 mu M) and compound L-3 had higher anti-HepG2 (1.63 mu M) and anti-MCF-7 (2.65 mu M) activities. Both of these compounds were recognized with high efficiency in apoptosis induction in HepG2 cells and intercalated binding modes with DNA. Moreover, with average IC50 values of 0.66 and 5.98 mu M, L-1 was nine times more effective at suppressing cultured HepG2 cells viability than normal cells (SI = 9). The relative tumor proliferation rate (T/C) was 38.6%, the tumor inhibition rate was up to 61.2%, which indicated that L-1 had no significant toxicity but high anti-HepG2 activity in vivo. Thus, it may be a potential antiproliferation drug with nontoxic side effects.

Safety of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Zhao, FY; Sun, X; Lu, W; Xu, L; Shi, JZ; Yang, SL; Zhou, MY; Su, F; Lin, F; Cao, FL or concate me.

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

In 2020 J ENZYM INHIB MED CH published article about PARKINSONS-DISEASE; DERIVATIVES; SAFINAMIDE; TARGETS; OPTIMIZATION; SEMBRAGILINE; PHARMACOLOGY; MODELS; POTENT in [Elkamhawy, Ahmed; Lee, Kyeong; Pae, Ae Nim; Park, Ki Duk] Dongguk Univ Seoul, Coll Pharm, Goyang 10326, South Korea; [Elkamhawy, Ahmed] Mansoura Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Mansoura, Egypt; [Paik, Sora; Roh, Eun Joo] Korea Inst Sci & Technol KIST, Chem Kin Res Ctr, Seoul 02792, South Korea; [Kim, Hyeon Jeong; Park, Jong-Hyun; Londhe, Ashwini M.] Korea Inst Sci & Technol KIST, Convergence Res Ctr Diag Treatment & Care Syst De, Seoul, South Korea; [Kim, Hyeon Jeong] Yonsei Univ, Dept Biotechnol, Seoul, South Korea; [Londhe, Ashwini M.; Pae, Ae Nim; Park, Ki Duk; Roh, Eun Joo] Korea Univ Sci & Technol, KIST Sch, Div Biomed Sci & Technol, Seoul, South Korea; [Park, Ki Duk] Kyung Hee Univ, KHU KIST Dept Converging Sci & Technol, Seoul, South Korea in 2020, Cited 52. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Computed Properties of C5H4N2O2

Herein, two new series ofN-substituted indole-based analogues were rationally designed, synthesizedviamicrowave heating technology, and evaluated as noteworthy MAO-B potential inhibitors. Compared to the reported indazole-based hitsVIandVII, compounds4band4eexhibited higher inhibitory activities over MAO-B with IC(50)values of 1.65 and 0.78 mu M, respectively. When compared to the modest selectivity index of rasagiline (II, a well-known MAO-B inhibitor, SI > 50), both4band4ealso showed better selectivity indices (SI > 60 and 120, respectively). A further kinetic evaluation of the most potent derivative (4e) displayed a competitive mode of inhibition (inhibition constant (K-i)/MAO-B = 94.52 nM). Reasonable explanations of the elicited biological activities were presentedviaSAR study and molecular docking simulation. Accordingly, the remarkable MAO-B inhibitory activity of4e(N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide), with its selectivity and competitive inhibition, advocates its potential role as a promising lead worthy of further optimization.

Computed Properties of C5H4N2O2. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Elkamhawy, A; Paik, S; Kim, HJ; Park, JH; Londhe, AM; Lee, K; Pae, AN; Park, KD; Roh, EJ or concate me.

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

An article Influence of the introduction of a triphenylphosphine group on the anticancer activity of a copper complex WOS:000564739400004 published article about IN-VITRO; MITOCHONDRIAL; CISPLATIN; DNA; LIGANDS; CYTOTOXICITY; MECHANISMS; CRYSTAL; DAMAGE; CELLS in [Zhao, Jin’an; Guo, Yan; Gan, Ning; Zhang, Junshuai; Hu, Jiyong] Henan Univ Urban Construct, Coll Mat & Chem Engn, Pingdingshan 467036, Henan, Peoples R China; [Li, Sen; Mei, Yameng; Yuan, Bangpeng; Hou, Hongwei] Zhengzhou Univ, Coll Chem, Zhengzhou 450001, Henan, Peoples R China in 2020, Cited 43. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. HPLC of Formula: C5H4N2O2

Aiming at obtaining new copper complexes with good cytotoxicity against cancer cells, triphenylphosphine (TPP) was introduced to obtain insight into the influence of the co-ligands. In this paper, two copper complexes, Cu(2-pbmq)(CH3OH)Br-2 (1) and [Cu(2-pbmq)(TPP)Br](2) (2) were designed, synthesized, and characterized by X-ray crystallography, 2-((2-(pyrazin-2-yl)-1H-benzo[d]imidazol-1-yl)methyl))quinolone (2-pbmq), to investigate the influence of the TPP group on the anticancer activity of the metal complex. Although the presence of the TPP group diminished the intensity of the interaction properties of the complex with DNA, the in vitro anticancer activity and cellular uptake of the TPP-containing complex were markedly superior to those of its TPP-lacking counterpart. Detailed studies on the more potently cytotoxic complex 2 revealed that it accumulated in nucleus, arrested the cell cycle at the G0-G1 phase, causing mitochondrial dysfunction, involving the potential simultaneous mitochondrial membrane collapse, cellular ATP level depletion, and Ca2+ leakage, eventually inducing cell apoptosis. In summary, the introduction of a TPP group enhances the biological activity and cytotoxicity of the complex.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Li, S; Zhao, JA; Guo, Y; Mei, YM; Yuan, BP; Gan, N; Zhang, JS; Hu, JY; Hou, HW or concate me.. HPLC of Formula: C5H4N2O2

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

In 2019 EUR J MED CHEM 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. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

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.

About Pyrazine-2-carboxylic acid, 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 concate me.. Formula: C5H4N2O2

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

Recently I am researching about MECHANISMS; IDENTIFICATION; INFLAMMASOME; CHEMOTAXIS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81573278, 81773745]; Excellent Science and Technology Innovation Team Projects of Jiangsu Province Universities in 2018; Double First-Class University project [CPU2018GF02]. Name: Pyrazine-2-carboxylic acid. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Zhang, ZG; Hao, K; Li, HW; Lu, R; Liu, CX; Zhou, MZ; Li, BY; Meng, ZB; Hu, QH; Jiang, C. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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.

Name: Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, 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 concate me.

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

In 2020 NAT COMMUN published article about ASPARTATE DECARBOXYLASE; SUSCEPTIBILITY; PANTOTHENATE; MUTATIONS; MODEL in [Sun, Qingan; Li, Xiaojun; Sacchettini, James C.] Texas A&M Univ, Dept Biochem & Biophys, College Stn, TX 77843 USA; [Perez, Lisa M.] Texas A&M Univ, Lab Mol Simulat, College Stn, TX USA; [Shi, Wanliang; Zhang, Ying] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Dept Mol Microbiol & Immunol, Baltimore, MD 21205 USA in 2020, Cited 30. 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

Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis. It is active against the persistent, non-replicating mycobacteria responsible for the protracted therapy required to cure tuberculosis. Pyrazinamide is a pro-drug that is converted into pyrazinoic acid (POA) by pyrazinamidase, however, the exact target of the drug has been difficult to determine. Here we show the enzyme PanD binds POA in its active site in a manner consistent with competitive inhibition. The active site is not directly accessible to the inhibitor, suggesting the protein must undergo a conformational change to bind the inhibitor. This is consistent with the slow binding kinetics we determined for POA. Drug-resistant mutations cluster near loops that lay on top of the active site. These resistant mutants show reduced affinity and residence time of POA consistent with a model where resistance occurs by destabilizing the closed conformation of the active site. The important tuberculosis drug pyrazinamide (PZA) is converted to its active form pyrazinoic acid (POA) in Mycobacterium tuberculosis (Mtb). Here the authors identify the pantothenate biosynthesis pathway enzyme aspartate decarboxylase (PanD) as the target of PZA and determine the POA bound Mtb PanD crystal structure.

Application In Synthesis of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Sun, QG; Li, XJ; Perez, LM; Shi, WL; Zhang, Y; Sacchettini, JC or concate me.

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

Recommanded Product: Pyrazine-2-carboxylic acid. Ragunathan, P; Cole, M; Latka, C; Aragaw, WW; Hegde, P; Shin, J; Manimekalai, MSS; Rishikesan, S; Aldrich, CC; Dick, T; Gruber, G in [Ragunathan, Priya; Latka, Chitra; Shin, Joon; Manimekalai, Malathy Sony Subramanian; Rishikesan, Sankaranarayanan; Gruber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore 637551, Singapore; [Cole, Malcolm; Hegde, Pooja; Aldrich, Courtney C.] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA; [Aragaw, Wassihun Wedajo; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Dick, Thomas] Hackensack Meridian Sch Med, Dept Med Sci, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20007 USA published Mycobacterium tuberculosis PanD Structure-Function Analysis and Identification of a Potent Pyrazinoic Acid-Derived Enzyme Inhibitor in 2021, Cited 28. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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.

About Pyrazine-2-carboxylic acid, 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 concate me.. Recommanded Product: Pyrazine-2-carboxylic acid

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

Cox, B; Duffy, J; Zdorichenko, V; Bellanger, C; Hurcum, J; Laleu, B; Booker-Milburn, KI; Elliott, LD; Robertson-Ralph, M; Swain, CJ; Bishop, SJ; Hallyburton, I; Anderson, M in [Duffy, James; Laleu, Benoit] Med Malaria Venture, CH-1215 Geneva 15, Switzerland; [Cox, Brian; Zdorichenko, Victor; Bellanger, Corentin; Bishop, Stephen J.] Univ Sussex, Photodivers Ltd, Sch Life Sci, Brighton BN1 9QJ, E Sussex, England; [Hurcum, Jessica] Univ Sussex, Sch Life Sci, Brighton BN1 9QJ, E Sussex, England; [Booker-Milburn, Kevin, I; Elliott, Luke D.] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England; [Booker-Milburn, Kevin, I; Robertson-Ralph, Michael] Univ Bristol, Sch Chem, Photodivers Ltd, Bristol BS8 1TS, Avon, England; [Swain, Christopher J.] Cambridge MedChem Consulting, Cambridge CB22 4RN, England; [Hallyburton, Irene; Anderson, Mark] Univ Dundee, Wellcome Ctr Antiinfect Res, Drug Discovery Unit, Dundee DD1 5EH, Scotland published Escaping from Flatland: Antimalarial Activity of sp(3)-Rich Bridged Pyrrolidine Derivatives in 2020, Cited 18. 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.

We utilized synthetic photochemistry to generate novel sp 3 -rich scaffolds and report the design, synthesis, and biological testing of a diverse series of amides based on the 1-(amino-methyl)-2-benzyl-2-azabicyclo[2.1.1]hexane scaffold. Preliminary antimalarial screening of the library provided promising compounds with activity in the 1-5 mu M range with an enhanced hit rate. Further evaluation (solubility, drug metabolism and pharmacokinetics (DMPK), and toxicity) of a selected compound (9) suggested that this series represents an excellent opportunity for further optimization with the framework offering multiple opportunities for the addition of uniquely vectorally positioned extra functionality.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Cox, B; Duffy, J; Zdorichenko, V; Bellanger, C; Hurcum, J; Laleu, B; Booker-Milburn, KI; Elliott, LD; Robertson-Ralph, M; Swain, CJ; Bishop, SJ; Hallyburton, I; Anderson, M or concate me.. Safety of Pyrazine-2-carboxylic acid

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

I found the field of Chemistry very interesting. Saw the article A chromone based Schiff base: An efficient colorimetric sensor for specific detection of Cu (II) ion in real water samples published in 2021. Application In Synthesis of Pyrazine-2-carboxylic acid, Reprint Addresses Malhotra, R (corresponding author), Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

A new chromone based Schiff base ligand L was synthesized by the condensation of 3-formyl chromone and pyrazine-2-carbohydrazide as a colorimetric probe to detect Cu (II) ions selectively. An instant visual colour change from colourless to yellow was obtained on addition of Cu2+ ions to the probe L solution, while other metal ions found ineffective. The ligand L was characterized by H-1 NMR, FTIR and HRMS spectral techniques. UV-Visible spectroscopic technique was used to study the sensing ability of probe L for copper ions above other metal ions. The Job’s plot obtained from absorption studies and HRMS data confirmed that the Cu2+ ions bind with ligand L in 1:1 stoichiometric ratio. DFT computations were also supported the binding framework between L and Cu (II) ions. The LOD value and the association constant were obtained 3.9 x 10(-7) M and 2.3 x 10(5) M-1 respectively, via Benesi-Hildebrand equation. Selectivity of L towards Cu2+ ions was also studied and it was found that the probe L worked specifically for copper ions without any considerable influence of other intruding metal ions. In addition, in real water samples, the ligand L was fully implemented for identification and quantification of Cu2+ ions. (C) 2020 Elsevier B.V. All rights reserved.

Application In Synthesis of Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Tomer, N; Goel, A; Ghule, VD; Malhotra, R or concate me.

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

Category: Pyrazines. Authors Yang, YJ; Wang, K; Yang, Y; Lai, FF; Chen, XG; Xiao, ZY in TAYLOR & FRANCIS LTD published article about in [Yang, Ya-Jun; Wang, Ke; Yang, Ying; Xiao, Zhi-Yan] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Active Subst Discovery & Druggabi, Beijing 100050, Peoples R China; [Lai, Fang-Fang; Chen, Xiao-Guang] 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 2021, Cited 21. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Based on the interaction modes of the natural 20S proteasome inhibitors TMC-95A, we have previously discovered a dipeptide 1. To explore the SAR around compound 1, we designed and synthesized a series of dipeptides (8-38) with a fragment-based strategy. Among them, nine compounds showed significant inhibitory activities against the chymotrypsin-like activity of human 20S proteasome with IC50 values at the submicromolar level, which were comparable or even superior to the parent compound 1. Meanwhile, they displayed no significant inhibition against trypsin-like and caspase-like activities of 20S proteasome. The results suggested the feasibility to design dipeptides as novel and potent 20S proteasome inhibitors.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Yang, YJ; Wang, K; Yang, Y; Lai, FF; Chen, XG; Xiao, ZY or concate me.. Category: Pyrazines

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