Tag: 100-200

Synthesis and biological evaluation of novel ‘CONH’ bridged indole and pyrazine derivatives was written by Kotnal, Ramaling B.. And the article was included in World Journal of Pharmaceutical Research in 2018.Safety of Ethyl pyrazine-2-carboxylate This article mentions the following:

A new series of N’-[(E)-Ph methylidene] pyrazine-2-carbohydrazide like 5-methyl-N’-[(1E)-(2-nitrophenyl)methylidene]pyrazine-2-carbohydrazide, N’-[(1E)-(2-hydroxyphenyl)methylidene]-5-methylpyrazine-2-carbohydrazide and N’-(2-oxo-1,2-dihydro-3H-indol-3-ylidene) pyrazine-2-carbohydrazide derivatives I (R = H, Me; R¹ = H, 5-CH₃, 7-F, 5-NO₂, 6-Br; R² = H, Me) were synthesized and evaluated for their antituberculosis, antibacterial and antifungal activities. All the synthesized compounds I were in good agreement with spectral anal. Three synthesized compounds I (R = Me, R¹ = F, R² = H; R = H, R¹ = F, R² = H; R = H, R¹ = 6-Br, R² = H) have shown significant anti-tubercular activity as compared to the reference drug. Compounds I (R = H, R¹ = 5-NO₂, R² = H; R = Me, R¹ = 5-NO₂, R² = H; R = H, R¹ = 6-Br, R² = H) shown good antibacterial activity against gram pos. bacteria and compounds I (R = H, R¹ = 7-F, R² = H; R = H, R¹ = 6-Br, R² = H) and 5-methyl-N’-[(1E)-(2-nitrophenyl)methylidene]pyrazine-2-carbohydrazide, N’-[(1E)-(2-hydroxyphenyl)methylidene]-5-methylpyrazine-2-carbohydrazide shown significant activity against gram neg. bacteria. Compounds I (R = Me, R¹ = F, R² = H; R = H, R¹ = 5-NO₂, R² = H; R = Me, R¹ = 6-Br, R² = H), 5-methyl-N’-[(1E)-(2-nitrophenyl)methylidene]pyrazine-2-carbohydrazide, N’-[(1E)-(2-hydroxyphenyl)methylidene]-5-methylpyrazine-2-carbohydrazide shown significant antifungal activity when compared with standard pyrazinamide, streptomycin, ciprofloxacin, fluconazole and were used as reference standard drug for the biol. activity, resp. The purity and structure confirmation of the synthesized compounds were done by TLC, IR and 1HNMR spectral study. In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Safety of Ethyl pyrazine-2-carboxylate).

Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) 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. A large number of pyrazine derivatives are known for their antitumor, antibiotic, anticonvulsant, antituberculosis, and diuretic activities.Safety of Ethyl pyrazine-2-carboxylate

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Polarographic reduction of the azines was written by Wiberg, Kenneth B.;Lewis, Thomas P.. And the article was included in Journal of the American Chemical Society in 1970.HPLC of Formula: 322-46-3 This article mentions the following:

The polarog. reduction of many azines is irreversible, with the initial anion radical undergoing rapid reaction to give other products. Cyclic voltammetry is able in most cases to effect reoxidation of the anion radical before it reacts further, and gives the reversible electrode potential. The observed energy differences between azine and radical anion are well correlated with the results of CNDO (complete neglect of differential overlap) and SCF π-electron calculations In the experiment, the researchers used many compounds, for example, Pyrido[2,3-b]pyrazine (cas: 322-46-3HPLC of Formula: 322-46-3).

Pyrido[2,3-b]pyrazine (cas: 322-46-3) 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. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.HPLC of Formula: 322-46-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

A Predictive Model Towards Site-Selective Metalations of Functionalized Heterocycles, Arenes, Olefins, and Alkanes using TMPZnCl·LiCl was written by Balkenhohl, Moritz;Jangra, Harish;Makarov, Ilya S.;Yang, Shu-Mei;Zipse, Hendrik;Knochel, Paul. And the article was included in Angewandte Chemie, International Edition in 2020.SDS of cas: 322-46-3 This article mentions the following:

The development of a predictive model towards site-selective deprotometalation reactions using TMPZnCl·LiCl is reported (TMP = 2,2,6,6-tetramethylpiperidinyl). The pK_a values of functionalized N-, S-, and O-heterocycles, arenes, alkenes, or alkanes were calculated and compared to the exptl. deprotonation sites. Large overlap (>80%) between the calculated and empirical deprotonation sites was observed, showing that thermodn. factors strongly govern the metalation regioselectivity. In the case of olefins, calculated frozen state energies of the deprotonated substrates allowed a more accurate prediction. Addnl., various new N-heterocycles were analyzed and the metalation regioselectivities rationalized using the predictive model. 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. Pyrazines are part of several biologically active polycyclic compounds; examples are quinoxalines, phenazines; and the bio-luminescent natural products pteridines, flavins, and their derivatives. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.SDS of cas: 322-46-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Hydrophobicity parameter of diazines IV: a new hydrogen-accepting parameter of monosubstituted (di)azines for the relationship of partition coefficients in different solvent systems was written by Yamagami, Chisako;Fujita, Toshio. And the article was included in Journal of Pharmaceutical Sciences in 2000.Name: Ethyl pyrazine-2-carboxylate This article mentions the following:

The authors recently proposed a new H-accepting scale, S_HA, for each member of the substituted (di)azine series from the heat of formation calculated under various dielec. environments by the COSMO method. The S_HA scale was used to examine relations between log P_CL (P_CL: CHCl₃/H₂O partition coefficient) and log P_oct (P_oct: 1-octanol/H₂O partition coefficient) for each of the 2-substituted pyridine (I), monosubstituted pyrazine (II), and pyrimidine (III) series. This S_HA parameter worked nicely, representing the H-accepting effect of the solute mol. A correlation equation with excellent quality, such as log P_CL = a log P_oct + sS_HA + constant, was obtained for each series. The authors further defined the parameter S_HA/PY, derived from S_HA values for the heterocyclic series by shifting the reference points to unsubstituted pyridine, to unify sep. derived correlation equations. Thus, the correlation between log P_CL and log P_oct for all combined data of three series was derived by using a single equation as log P_CL = a log P_oct + sS_HA/PY + constant The S_HA parameters were reasonably considered as being free-energy related, and the rationale for the H-bond-acceptor scale was presented. In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Name: Ethyl pyrazine-2-carboxylate).

Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) 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. Substituted pyrazines have been found as subunits of multiple synthetically constructed therapeutic agents, as well as several natural products.Name: Ethyl pyrazine-2-carboxylate

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Substituted pyrido[2,3-b]pyrazines was written by Kaye, Irving A.. And the article was included in Journal of Medicinal Chemistry in 1964.Electric Literature of C7H5N3 This article mentions the following:

Pyrido[2,3-b]pyrazines were prepared by condensing 2,3-diaminopyridine or 2,3,6-triaminopyridine with an α-diketone or (CO₂Et)₂; Pb 6-aminopyrido[2,3-b]pyrazine-2,3-dicarboxylate was obtained by KMnO₄ oxidation of 6-amino-2,3-dimethylpyrido[2,3-b]pyrazine. In the experiment, the researchers used many compounds, for example, Pyrido[2,3-b]pyrazine (cas: 322-46-3Electric Literature of C7H5N3).

Pyrido[2,3-b]pyrazine (cas: 322-46-3) 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). Pyrazines are chemical compounds (technically called “methoxypyrazines”) found in grape skin and stems that are responsible for many “green” flavors in wine. Levels of pyrazines are dependent on viticultural practices, climate, and grape variety.Electric Literature of C7H5N3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Alkylamino derivatives of pyrazinamide: Synthesis and antimycobacterial evaluation was written by Servusova, Barbora;Paterova, Pavla;Mandikova, Jana;Kubicek, Vladimir;Kucera, Radim;Kunes, Jiri;Dolezal, Martin;Zitko, Jan. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Synthetic Route of C5H6N4O This article mentions the following:

A series of pyrazinamide derivatives with alkylamino substitution was designed, synthesized and tested for their ability to inhibit the growth of selected mycobacterial, bacterial and fungal strains. The target structures were prepared from the corresponding 5-chloro or 6-chloropyrazine-2-carboxamide by nucleophilic substitution of chlorine by various non-aromatic amines (alkylamines). To determine the influence of alkyl substitution, corresponding amino derivatives and compounds with phenylalkylamino substitution were prepared Some of the compounds exerted antimycobacterial activity against Mycobacterium tuberculosis H37Rv significantly better than standard pyrazinamide and corresponding starting compounds Basic structure-activity relations are presented. Only weak antibacterial and no antifungal activity was detected. In the experiment, the researchers used many compounds, for example, 5-Aminopyrazine-2-carboxamide (cas: 89323-09-1Synthetic Route of C5H6N4O).

5-Aminopyrazine-2-carboxamide (cas: 89323-09-1) belongs to pyrazine derivatives. Pyrazine has the elements of symmetry for the point group D2h. It has three mutually perpendicular two-fold axes. It also has three mutually perpendicular planes of symmetry. As a result, pyrazine also has a centre of symmetry. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Synthetic Route of C5H6N4O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity was written by Yang, Xiao-Zhi;Yang, Wen-Hui;Xu, Yun-Gen;Diao, Xiao-Juan;He, Guang-Wei;Gong, Guo-Qing. And the article was included in European Journal of Medicinal Chemistry in 2012.Formula: C8H12N2O This article mentions the following:

A novel series of prodrugs I(R = tBu, hexyl, pentyl, iPr, Et, Bn, Me) consisting of dabigatran and 2-hydroxymethyl-3,5,6-trimethylpyrazine (HTMP) were synthesized. The pharmacol. results show that all of them possess the effect of anti-platelet aggregation induced by thrombin in vitro. Moreover, one of those compounds, I(R = hexyl) (ED₅₀ = 2.1 ± 1.3 mg/kg) shows more potent activity for inhibiting thrombosis in vivo than that of dabigatran etexilate (ED₅₀ = 4.4 ± 2.2 mg/kg). In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Formula: C8H12N2O).

(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. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.Formula: C8H12N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Design, synthesis, in vitro and in vivo evaluation against MRSA and molecular docking studies of novel pleuromutilin derivatives bearing 1, 3, 4-oxadiazole linker was written by Liu, Jie;Zhang, Guang-Yu;Zhang, Zhe;Li, Bo;Chai, Fei;Wang, Qi;Zhou, Zi-Dan;Xu, Ling-Ling;Wang, Shou-Kai;Jin, Zhen;Tang, You-Zhi. And the article was included in Bioorganic Chemistry in 2021.Safety of Ethyl pyrazine-2-carboxylate This article mentions the following:

A class of pleuromutilin derivatives containing 1,3,4-oxadiazole were designed and synthesized as potential antibacterial agents against Methicillin-resistant staphylococcus aureus (MRSA). The ultrasound-assisted reaction was proposed as a green chem. method to synthesize 1,3,4-oxadiazole derivatives Among these pleuromutilin derivatives, compound 133 (I) was found to be the strongest antibacterial derivative against MRSA (MIC = 0.125μg/mL). Furthermore, the result of the time-kill curves displayed that compound 133 could inhibit the growth of MRSA in vitro quickly (-4.36 log10 CFU/mL reduction). Then, compound 133 (-1.82 log₁₀ CFU/mL) displayed superior in vivo antibacterial efficacy than tiamulin (-0.82 log₁₀ CFU/mL) in reducing MRSA load in mice thigh model. Besides, compound 133 exhibited low cytotoxicity to RAW 264.7 cells. Mol. docking studies revealed that compound 133 was successfully localized in the binding pocket of 50S ribosomal subunit (ΔG_b = -10.50 kcal/mol). The results indicated that these pleuromutilin derivatives containing 1,3,4-oxadiazole might be further developed into novel antibiotics against MRSA. In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Safety of Ethyl pyrazine-2-carboxylate).

Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. 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.Safety of Ethyl pyrazine-2-carboxylate

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthesis and characterization of Ligustrazine-piperazidine derivatives was written by Xue, Peng;Lv, Guo-kai;Cheng, Xian-chao;Liu, Xin-yong. And the article was included in Huaxue Shiji in 2006.Related Products of 75907-74-3 This article mentions the following:

Four Ligustrazine-piperazidine derivatives were synthesized from Ligustrazine hydrate, followed by oxidation, acylation, hydrolysis, halogenation, and alkylation, their chem. structures were characterized by IR, ¹H NMR and MS. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Related Products of 75907-74-3).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, α-hydroxyketone, α-methyl ketone. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.Related Products of 75907-74-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthesis, oxidation potential and anti-mycobacterial activity of isoniazid and analogues: insights into the molecular isoniazid activation mechanism was written by Laborde, Julie;Deraeve, Celine;Lecoq, Lea;Sournia-Saquet, Alix;Stigliani, Jean-Luc;Orena, Beatrice S.;Mori, Giorgia;Pratviel, Genevieve;Bernardes-Genisson, Vania. And the article was included in ChemistrySelect in 2016.Category: pyrazines This article mentions the following:

In this work, a series of 21 INH analogs e.g., pyridine-2-carbohydrazide was synthesized, their oxidation potentials were determined and their anti-mycobacterial activities were evaluated against MTB wild-type and resistant strains. On the contrary to what was postulated, no correlation exists between the easier oxidation of a mol. and its anti-MTB activity toward resistant strains. Based on exptl. data and theor. calculations, an activation mechanism for INH and analogs has been proposed, based on a one-electron oxidation step. It first involves the oxidation of hydrazyl function at the proximal nitrogen followed by a radical transposition to the distal nitrogen, which then induces a β-homolytic cleavage of the C(=O)-N bond to afford diazene and the isonicotinoyl radical species. In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Category: pyrazines).

Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem