Tag: 100-200

Synthesis and anti-platelet aggregation activity evaluation of ligustrazine derivatives was written by Fan, Lingling;Li, Yi;Wu, Xiaofang;Li, Yong;Zhang, Jue. And the article was included in Huaxue Tongbao in 2018.Safety of (3,5,6-Trimethylpyrazin-2-yl)methanol This article mentions the following:

Using ligustrazine (TMP) and o-phenylenediamine as raw materials, seven derivatives were synthesized via KMnO₄ oxidation, esterification, cyclization and reduction The structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. The in vitro anti-platelet aggregation activities of the target compounds have been preliminarily tested by the Born turbidimetric method, and the exptl. results showed that compounds 3 (IC₅₀ = 0.23 mmol/L) and 7 (IC₅₀ = 0.27mmol/L) have significant inhibitory activity of against ADP (ADP) induced platelet aggregation, higher than that of ligustrazine (IC₅₀ = 0.42mmol/L). In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Safety of (3,5,6-Trimethylpyrazin-2-yl)methanol).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazines are part of several biologically active polycyclic compounds; examples are quinoxalines, phenazines; and the bio-luminescent natural products pteridines, flavins, and their derivatives. Pyrazines undergo nearly all of the same reactions as pyrimidines, from nucleophilic substitution (SNAr) to palladium-catalyzed cross coupling reactions.Safety of (3,5,6-Trimethylpyrazin-2-yl)methanol

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke was written by Sun, Yewei;Jiang, Jie;Zhang, Zaijun;Yu, Pei;Wang, Linda;Xu, Changlin;Liu, Wei;Wang, Yuqiang. And the article was included in Bioorganic & Medicinal Chemistry in 2008.COA of Formula: C8H12N2O This article mentions the following:

Ischemic stroke results from brain blood vessel blockage by thrombus, and produces neuronal cell damage and death. While thrombolytic therapy with tPA has achieved some success in clinic, the strategy of using neuroprotective agents to treat ischemic stroke has been disappointing thus far. In the present work, the authors synthesized TBN, a derivative of the clin. useful stroke drug TMP armed with a powerful free radical-scavenging nitrone moiety. TBN retains the thrombolytic activity of the parent TMP and possesses strong antioxidative properties. TBN demonstrates significant activity in the rat MCAo stroke model. The results suggest that design of mols. possessing both thrombolytic and neuroprotective properties may be a novel strategy for effective stroke therapeutics. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3COA of Formula: C8H12N2O).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazinesare six-membered aromatic heterocyclic organic compounds with two nitrogen atoms at 1,4-positions. Pyrazine is a weaker base (pKb = 13.4) than pyridine (pKb = 8.8), pyrimidine (pKb = 12.7). A large number of pyrazine derivatives are known for their antitumor, antibiotic, anticonvulsant, antituberculosis, and diuretic activities.COA of Formula: C8H12N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Preparation and investigation of the spectral and electrochemical properties of mixed-ligand ruthenium(II) complexes containing 1,8-naphthyridines was written by Staniewicz, Robert J.;Sympson, Robert F.;Hendricker, David G.. And the article was included in Inorganic Chemistry in 1977.Related Products of 322-46-3 This article mentions the following:

Mixed-ligand complexes of the form Ru(bpy)2L2+ and Ru(phen)2L2+, L = 1,8-naphthyridine (napy), 2,7-dimethyl-1,3-naphthyridine, 2-methyl-1,8-naphthyridine, and pyrido[2,3-b]pyrazine, and bpy is 2,2′-bipyridine and phen is 1,10-phenanetroline were prepared and isolated as their PF6- salts. The formulations were confirmed by elemental and anal. and conductivity measurements while the purity of the compounds was judged by the single maximum observed in the a.c. polarograms. The solution spectra of the mixed-ligand complexes are characterized by a high-intensity (ε âˆ?04) metal-to-ligand charge-transfer band at âˆ?50 nm and π â†?π* intraligand UV transitions. The energies and intensities of these absorptions are compared with previously reported Ru(byp)2X22+ complexes. The reduction potentials (Ru3+/Ru2+) for the napy mixed-ligand complexes were determined using both cyclic voltammetry and a.c. polarog. and the reversibility of the electrochem. couples was established. The E1/2 values do not vary greatly from those observed for the (phen)3- and (bpy)3Ru(II) complexes thus indicating that the stability of the Ru(II) state has not been significantly altered by the replacement of a phen or bpy with a napy type ligand. In the experiment, the researchers used many compounds, for example, Pyrido[2,3-b]pyrazine (cas: 322-46-3Related Products of 322-46-3).

Pyrido[2,3-b]pyrazine (cas: 322-46-3) belongs to pyrazine derivatives. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Related Products of 322-46-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ligustrazine derivatives. Part 4: Design, synthesis, and biological evaluation of novel ligustrazine-based stilbene derivatives as potential cardiovascular agents was written by Deng, Lijuan;Guo, Xiuli;Zhai, Li;Song, Yuning;Chen, Hongfei;Zhan, Peng;Wu, Jingde;Liu, Xinyong. And the article was included in Chemical Biology & Drug Design in 2012.Quality Control of (3,5,6-Trimethylpyrazin-2-yl)methanol This article mentions the following:

A series of novel stilbene derivatives containing ligustrazinyl moiety was designed, synthesized, and assayed for their protective effects on damaged endothelial cells. The results showed that most ligustrazinyl stilbene derivatives exhibited high protective effects on the human umbilical vascular endothelial cells (HUVECs) damaged by hydrogen peroxide in comparison with Ligustrazine. Structure-activity relationships were briefly discussed. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Quality Control of (3,5,6-Trimethylpyrazin-2-yl)methanol).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine derivatives have antitumor, antibiotic, anticonvulsant, antituberculous and diuretic effects as well as kinase, enzymatic and potent tubulin and FtsZ polymerization inhibitory activities. Pyrazines undergo nearly all of the same reactions as pyrimidines, from nucleophilic substitution (SNAr) to palladium-catalyzed cross coupling reactions.Quality Control of (3,5,6-Trimethylpyrazin-2-yl)methanol

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Calculation of electronic spectra of azabenzenes and azanaphthalenes by a simplified version of the Pariser-Parr-Pople method was written by Favini, Giorgio;Vandoni, Ida;Simonetta, Massimo. And the article was included in Theoretica Chimica Acta in 1965.SDS of cas: 322-46-3 This article mentions the following:

The simplified version given by Heilbronner, et al. (CA 60, 15160h) of the Pariser-Parr-Pople treatment was used to calculate transition energies and intensities of the π – π^* bands in the electronic spectra of 31 azines (azabenzenes and azanaphthalenes). A comparison with exptl. data results in a better agreement than for the complete treatment. In the experiment, the researchers used many compounds, for example, Pyrido[2,3-b]pyrazine (cas: 322-46-3SDS of cas: 322-46-3).

Pyrido[2,3-b]pyrazine (cas: 322-46-3) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes.SDS of cas: 322-46-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ligustrazine derivatives. Part 3: Design, synthesis and evaluation of novel acylpiperazinyl derivatives as potential cerebrocardiac vascular agents was written by Cheng, Xian-Chao;Liu, Xin-Yong;Xu, Wen-Fang;Guo, Xiu-Li;Zhang, Ning;Song, Yu-Ning. And the article was included in Bioorganic & Medicinal Chemistry in 2009.SDS of cas: 75907-74-3 This article mentions the following:

A series of novel acylpiperazinyl Ligustrazine derivatives was designed, synthesized, and their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities were evaluated. The results showed that compound I (R = salicyloyl) displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound I (R = acetylsalicyloyl) was found to be the most active antiplatelet aggregation agent. Structure-activity relationships were briefly discussed. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3SDS of cas: 75907-74-3).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.SDS of cas: 75907-74-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

A platform for designing HIV integrase inhibitors. 2-Hydroxy-3-heteroaryl acrylic acid derivatives as novel HIV integrase inhibitor and modeling of hydrophilic and hydrophobic pharmacophores was written by Kawasuji, Takashi;Yoshinaga, Tomokazu;Sato, Akihiko;Yodo, Mitsuaki;Fujiwara, Tamio;Kiyama, Ryuichi. And the article was included in Bioorganic & Medicinal Chemistry in 2006.Synthetic Route of C7H8N2O2 This article mentions the following:

The authors present a novel series of HIV integrase inhibitors, showing IC₅₀s ranging from 0.01 to over 370 μM in an enzymic assay. Furthermore, pharmacophore modeling study for the inhibitors was carried out to elucidate the structure-activity relationships. Finally, the authors found a 3D-pharmacophore model, which is composed of a hydrophilic and a hydrophobic domain, providing valuable information for designing other novel types of integrase inhibitors. In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Synthetic Route of C7H8N2O2).

Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. Pyrazines undergo nearly all of the same reactions as pyrimidines, from nucleophilic substitution (SNAr) to palladium-catalyzed cross coupling reactions.Synthetic Route of C7H8N2O2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

A systems biology approach to understanding the mechanisms of action of Chinese herbs for treatment of cardiovascular disease was written by Li, Bohui;Xu, Xue;Wang, Xia;Yu, Hua;Li, Xiuxiu;Tao, Weiyang;Wang, Yonghua;Yang, Ling. And the article was included in International Journal of Molecular Sciences in 2012.Synthetic Route of C8H12N2O This article mentions the following:

Traditional Chinese Medicine (TCM) involves a broad range of empirical testing and refinement and plays an important role in the health maintenance for people all over the world. However, due to the complexity of Chinese herbs, a full understanding of TCM’s action mechanisms is still unavailable despite plenty of successful applications of TCM in the treatment of various diseases, including especially cardiovascular diseases (CVD), one of the leading causes of death. Thus in the present work, by incorporating the chem. predictors, target predictors and network construction approaches, an integrated system of TCM has been constructed to systematically uncover the underlying action mechanisms of TCM. From three representative Chinese herbs, i.e., Ligusticum chuanxiong Hort., Dalbergia odorifera T. Chen and Corydalis yanhusuo WT Wang which have been widely used in CVD treatment, by combinational use of drug absorption, distribution, metabolism and excretion (ADME) screening and network pharmacol. techniques, we have generated 64 bioactive ingredients and identified 54 protein targets closely associated with CVD, of which 29 are common targets (52.7%) of the three herbs. The result provides new information on the efficiency of the Chinese herbs for the treatment of CVD and also explains one of the basic theories of TCM, i.e., “multiple herbal drugs can treat one disease”. The predicted potential targets were then mapped to target-disease and target-signal pathway connections, which revealed the relationships of the active ingredients with their potential targets, diseases and signal systems. This means that for the first time, the action mechanism of these three important Chinese herbs for the treatment of CVD is uncovered, by generating and identifying both their active ingredients and novel targets specifically related to CVD, which clarifies some of the common conceptions in TCM, and thus provides clues to modernize such specific herbal medicines. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Synthetic Route of C8H12N2O).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes.Synthetic Route of C8H12N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthesis and evaluation of new chalcones and oximes as anticancer agents was written by Bukhari, Syed Nasir Abbas. And the article was included in RSC Advances in 2022.Category: pyrazines This article mentions the following:

Complex illnesses, such as cancer, are often caused by many disorders, gene mutations, or pathways. Biol. pathways play a significant part in the development of these diseases. Multi-target directed ligands (MTDLs) have been used by medicinal chemists recently in an effort to find single mols. that can affect many targets concurrently. In this work, several chalcones containing the ligustrazine moiety were synthesized and tested for their in vitro anticancer activity and several cancer markers, including EGFR, BRAF^V600E, c-Met, and tubulin polymerization, in order to uncover multitarget bioactive compounds In assays using multiple cancer cell lines, the majority of the compounds examined showed strong anticancer activity against them. To synthesize oximes, all of the chalcones were used as precursors. The IC₅₀ values of two compounds ((1Z,2E)-1-(4-(5-Bromothiophen-2-yl)phenyl)-3-(3,5,6-trimethylpyrazin-2-yl)prop-2-en-1-one oxime and (1Z,2E)-1-(4-(4-Methylthiophen-2-yl)phenyl)-3-(3,5,6-trimethylpyrazin-2-yl)prop-2-en-1-one oxime) were found to be 0.87, 0.28, 2.43, 1.04 μM and (1Z,2E)-1-(4-(Thiophen-2-yl)phenyl)-3-(3,5,6-trimethylpyrazin-2-yl)prop-2-en-1-one oxime, 1.47, 0.79, 3.8, 1.63 μM resp., against A-375, MCF-7, HT-29 and H-460 cell lines. These IC₅₀ values revealed an excellent antiproliferative activity compared to those of the pos. control foretinib, (IC₅₀ = 1.9, 1.15, 3.97, and 2.86 μM). Careful examination of their structure and configuration revealed that both compounds had an oxime functional group with z configuration, in place of carbonyl functional group, along with a 2-Ph thiophenyl moiety with or without a bromo group at position-5. The possible binding pattern was implied by docking simulation, inferring the possibility of introducing interactions with the nearby tubulin chain. Since the novel structural trial has been conducted with a detailed structure activity relationship discussion, this work might stimulate new ideas in further modification of multitarget anti-cancer agents and therapeutic approaches. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Category: pyrazines).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. A large number of pyrazine derivatives are known for their antitumor, antibiotic, anticonvulsant, antituberculosis, and diuretic activities.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Cinnolines. IV. Quaternization of 4-amino-6-chloro- and 6-chloro-4-phenoxycinnoline was written by Ames, D. E.. And the article was included in Journal of the Chemical Society in 1964.Name: 5-Aminopyrazine-2-carboxamide This article mentions the following:

The work of Simpson (CA 42, 2978e) on the quaternization of 4-amino-6-chlorocinnoline (I) has been reexamined, and alkylation is shown to occur at N-1 and N-2 on the basis of revised structures for the methylation products of 6-chloro-4-hydroxycinnoline. 6-Chloro-4-phenoxycinnoline, however, appears to form a methiodide only by reaction at N-2. In the experiment, the researchers used many compounds, for example, 5-Aminopyrazine-2-carboxamide (cas: 89323-09-1Name: 5-Aminopyrazine-2-carboxamide).

5-Aminopyrazine-2-carboxamide (cas: 89323-09-1) belongs to pyrazine derivatives. Pyrazines are part of several biologically active polycyclic compounds; examples are quinoxalines, phenazines; and the bio-luminescent natural products pteridines, flavins, and their derivatives. Substituted pyrazines have been found as subunits of multiple synthetically constructed therapeutic agents, as well as several natural products.Name: 5-Aminopyrazine-2-carboxamide

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem